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DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 36Yrs Exp. in the feld of Organic Chemistry,Working for AFRICURE PHARMA as ADVISOR earlier with GLENMARK PHARMA at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google, NO ADVERTISEMENTS , ACADEMIC , NON COMMERCIAL SITE, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution, ........amcrasto@gmail.com..........+91 9323115463, Skype amcrasto64

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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How to identify Out-of-Trend Results in Stability Studies?

September 25, 2014 7:44 am / Leave a comment

DRUG REGULATORY AFFAIRS INTERNATIONAL

How to identify Out-of-Trend Results in Stability Studies?
http://www.gmp-compliance.org/enews_4522_How-to-identify-Out-of-Trend-Results-in-Stability-Studies_8360,8348,8430,Z-QCM_n.html

An article in PharmTech from June 2013 (by Trajkovic-Jolevska et. al) deals with the methods to identify Out-of-Trend (OOT) results in ongoing stability studies.

With regard to stability studies, it is important to make the difference between Out-of-Specification (OOS) and Out-of-Trend (OOT). Both the pharmaceutical industry and authorities often misuse these two terms.

The article defines OOT results as those results which don’t follow the expected trend, either in comparison with other stability batches or compared to previous results collected during a stability study. OOT results aren’t necessarily OOS, but they don’t look like a typical data point.
Although OOT results are a serious problem, neither the scientific literature nor regulatory guidelines fully address them.

The aim of the study described in this Pharmtech article by Trajkovic-Jolevska et. al was to perform a statistical evaluation of the statistical methods used in…

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Pirenperone, R 47465

September 25, 2014 7:33 am / Leave a comment

Figure imgf000044_0003

ON THE LEFT OR ABOVE

3-(2- {4-[(4-fluorophenyl)carbonyl]piperidin- 1 -yl} ethyl)-2-methyl-4H-pyrido[ 1 ,2- α]pyrimidin-4-one

3-(2-{4-[(4-fluorophenyl)carbonyl]piperidin-1-yl}ethyl)-2-methyl-4H-pyrido[1,2-α]pyrimidin-4-one

3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2-methyl-4H-pyrido[1,2-a]pyri- midin-4-one

pirenperone CAS : 75444-65-4

C₂₃ H₂₄ F N₃ O₂

4H-Pyrido[1,2-a]pyrimidin-4-one, 3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2-methyl-

R 47465

Cardiovascular disease; Inflammatory disease; Neoplasm; Pain

Calcium channel modulator T-type

……………………………..

http://www.google.co.in/patents/US4342870

http://www.google.co.in/patents/EP0037265A1

Example XXIV

A solution of 2 parts of 3-[2-[4-(4-fluorobenzoyl)-1 -piperidinyl]ethyl]-2 -methyl-4H -pyricio[1, 2 -a]pyrimidin-4-one in 64 parts of 2-propanol is warm acidified with 2-propanol saturated with hydrogen chloride. The formed hydrochloride salt is allowed to crystallize. It is filtered off and dried, yielding 2 parts (85. 5%) of 3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2-methyl-4H-pyrido[1,2-a]pyri- midin-4-one dihydrochloride; mp. + 300°C.
In a similar manner there are also prepared:
- 3-[2 -[4-(4-fluorobenzoyl)-1-piperidiny]yethyl7-2 -methyl-4H-pyrido-[1, 2 -a]pyrimidin-4-one sulfate (1 : 2); mp. 254. 7°C; and
- 3-[2-[4-(4-fluorobenzoyl)-1 -piperidinyl]ethyl]-2-methyl-4H-pyrido-[1, 2-a]pyrimidin-4-one phosphate (1 : 2) ; mp. 243.8°C.

WO-2014143915

http://www.google.com/patents/WO2014143915A1?cl=en

Vm Therapeutics Llc

Novelcrystalline polymorphic forms of pirenperone, useful for treating disorders associated with T-type calcium ion channels such as pain syndrome, neoplasm, cardiovascular disease or inflammation. VM Discovery, from which VM Therapeutics was spun out, was investigating the VMD-C300 series of compounds which act as T-type calcium channel modulators, including VMD-3816 and VMD-3222, for treating cancer, pain, neurological diseases and cardiovascular diseases; but as of September 2014, this program was assumed to be discontinued. See WO2009108798, (by the inventor, assigned to VM Discovery) claiming use of the same compound for treating same indications.

It was first disclosed in the now-expired US Patent No. 4,342,870 (Claim 5), and intended to be used as potential anti-anxiety drug. However, the early human clinical studies has shown that the compound did not show any dose-related anti-anxiety effects as hoped, but otherwise the compound was safe in human (ref. Ansseau M, Doumo t A, Thlry D, Gelders Y. “Pilot study of a specific serotonergic antagonist, pirenperone, in the treatment of anxiety disorders”, Acta Psychiatr Belg, 1983 Sep-Oct;83(5):517-24). in the US Patent No. 4,342,870, there is no crystalline polymorphic form disclosed, nor disclosure of potential uses for management of pain and treatment of other related diseases or disorders.

It was further disclosed in the PCT patent application WO/2009/108798 as “Compound 10 (pirenperone)^‘” to be used for novel T-type calcium ion channel antagonist for management of pain and treatment of other diseases or disorders associated to the T-type calcium ion channels.

Surprisingly, we have found that there are many crystalline polymorphic forms of this compound which may affect the compound’s pharmaceutical safety and pharmacology properties.

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Amgen files ‘breakthrough’ leukaemia drug Blinatumomab (AMG103) in the US

September 25, 2014 6:57 am / 1 Comment on Amgen files ‘breakthrough’ leukaemia drug Blinatumomab (AMG103) in the US

Blinatumomab

Biotechnology giant Amgen has filed its investigational cancer immunotherapy blinatumomab in the US for the treatment of certain forms of acute lymphoblastic leukaemia (ALL).

Specifically, the Biologic License Application seeks approval to market the drug for patients with Philadelphia-negative (Ph-) relapsed/refractory B-precursor forms of the aggressive blood/bone marrow cancer.

Structure and mechanism of action

Blinatumomab linking a T cell to a malignant B cell.

Blinatumomab enables a patient’s T cells to recognize malignant B cells. A molecule of blinatumomab combines two binding sites: a CD3 site for T cells and a CD19 site for the target B cells. CD3 is part of the T cell receptor. The drug works by linking these two cell types and activating the T cell to exert cytotoxic activity on the target cell.^[2]

Therapeutic use

Clinical trials

In a phase 1 clinical study with blinatumomab, patients with non-Hodgkin’s lymphoma showed tumor regression, and in some cases completeremission.^[3] There are ongoing phase 1 and phase 2 clinical trials of blinatumomab in patients with acute lymphoblastic leukemia (ALL),^[4]lung or gastrointestinal cancers.^{[citation needed]} One phase II trial for ALL reported good results in 2010 and another is starting.^[5]

Blinatumomab
Monoclonal antibody
Type	Bi-specific T-cell engager
Source	Mouse
Target	CD19, CD3
Clinical data
Legal status	?
Identifiers
CAS number	853426-35-4
ATC code	None
UNII	4FR53SIF3A
Chemical data
Formula	C₂₃₆₇H₃₅₇₇N₆₄₉O₇₇₂S₁₉
Mol. mass	54.1 kDa

References

Statement on a Nonproprietary Name adopted by the USAN Council: Blinatumomab
Mølhøj, M; Crommer, S; Brischwein, K; Rau, D; Sriskandarajah, M; Hoffmann, P; Kufer, P; Hofmeister, R; Baeuerle, PA (March 2007). “CD19-/CD3-bispecific antibody of the BiTE class is far superior to tandem diabody with respect to redirected tumor cell lysis”. Mol Immunol 44 (8): 1935–43. doi:10.1016/j.molimm.2006.09.032. PMID 17083975.
Bargou, R; et al. (2008). “Tumor regression in cancer patients by very low doses of a T cell-engaging antibody”. Science 321 (5891): 974–977. doi:10.1126/science.1158545.PMID 18703743.
ClinicalTrials.gov NCT00560794 Phase II Study of the BiTE Blinatumomab (MT103) in Patients With Minimal Residual Disease of B-precursor Acute ALL
“Micromet initiates MT103 phase 2 trial in adult ALL patients”. 20 Sep 2010.

External links

Clinical trials of blinatumomab

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Pharmaceuticals; Make in India

September 25, 2014 3:59 am / 1 Comment on Pharmaceuticals; Make in India

Indian PM Narendra Modi: Understanding an enigma PM, MODI
Brand India Pharma aims to make the most of a booming domestic pharma industry
India’s pharma exports stood at 90,000 crore rupees ($15 billion) for the year 2013-2014, and are set to cross the 1 lakh crore rupees ($16.4 billion) mark in the current financial year. The Brand India Pharma campaign aims to tap into this value proposition, under the guidance of the Indian Ministry of Commerce and Industry, aiming to showcase the strengths of the Indian pharma industry.

With more than 10,500 manufacturing units and more than 3,000 pharma companies, India is ranked among the top six producers of pharmaceuticals worldwide, and is well-positioned to take advantage of its place in a global landscape.

READ AT

http://www.thepharmaletter.com/article/brand-india-pharma-aims-to-make-the-most-of-a-booming-domestic-pharma-industry

List of WHO Approved Pharma Plant in India

http://pharmatips.doyouknow.in/Articles/Pharma-Companies/List-Of-WHO-Approved-Pharma-Plant-In-India.aspx

India’s spacecraft cost $74 million, a fraction of the $671 million spent by NASA’s MAVEN ……….SEPT 24 2014

Indian Pharma Sector

India is already among the top six producers of pharmaceuticals of the world. The Government of India has announced a host of measures to create a facilitating environment for the Indian pharmaceutical industry. The policies of the Government of India are aimed at building more hospitals, boosting local access to healthcare, improving the quality of medical training, increasing public expenditure on healthcare to 2-3 per cent of GDP, up from the current level of 1 per cent. At the same time, the growth in healthcare insurance industry in India is also expected to complement the overall growth in the pharmaceutical market.

READ AT

http://www.brandindiapharma.in/infographic-business/

India’s spacecraft reaches Mars orbit … and history

India’s spacecraft cost $74 million, a fraction of the $671 million spent by NASA’s MAVEN

24 sept 2014

India’s Mars Orbiter Mission successfully entered Mars’ orbit Wednesday morning, becoming the first nation to arrive on its first attempt and the first Asian country to reach the Red Planet.

“We have gone beyond the boundaries of human enterprise and human imagination,” declared India’s Prime Minister Narendra Modi, who watched from the space agency’s nerve center in Bangalore. “We have accurately navigated our spacecraft through a route known to a very few.”

The staff at the Indian Space Research Organization erupted into applause and cheers after learning that the Mars Orbiter Mission, also known as Mangalyaan, reached the planet’s orbit and made history.

Before Wednesday, only the United States, Europe and the Soviets have successfully sent spacecraft to Mars.

$India\'s space agency and Prime Minister Narendra Modi cheer the Mars mission.$

India’s space agency and Prime Minister Narendra Modi cheer the Mars mission.

$Photos: India\'s first Mars orbiter$ Photos: India’s first Mars orbiter

“The odds were stacked against us,” Modi said. “Of the 51 missions attempted so far, a mere 21 had succeeded. But we have prevailed.”

And India reached Mars with significantly less money.

With a price tag of $74 million, the Mars Orbiter Mission cost a mere fraction of the $671 million NASA spent on its MAVEN spacecraft, which arrived to Mars earlier this week. Some space observers noted that India’s Mars orbiter cost less than the $100 million budget for the space thriller film “Gravity.”

Interactive: Exploring Mars from Viking to MAVEN

“It shows how optimal is the design, that way we’re able to cut cost and we’re not compromising quality,” said S. Satish, a space expert based in Bangalore.

The groundbreaking Mars mission wasn’t without controversy — with some critics who said India should spend the money on other issues.

The spacecraft launched on November 5, and has traveled over 650 million kilometers to enter Mars orbit. Its mission is to orbit the Red Planet, mapping its surface and studying the atmosphere. The Mars Orbiter kicked off its interplanetary debut with its own Twitter account.

The mission has been freighted with patriotic significance for India since its inception and is seen as a symbolic coup over its rival, China, which is also ramping up its space ambitions.

India launches mission to Mars

China’s joint mission with Russia in 2011, which contained the Chinese Mars satellite Yinhuo-1, stalled and eventually fell back to Earth. Japan’s 1998 attempt with the spacecraft Nozomi was also unsuccessful due to fuel problems.

Once nears Mars’ orbit, India’s spacecraft had to execute a series of complicated and critical maneuvers. About half of all spacecraft sent on missions to the planet have veered off course, malfunctioned or crashed.

India’s Mars Orbiter Mission is in the company of NASA’s two Mars rovers on the ground, a European orbiter and NASA orbiters including the MAVEN, which has been there since Sunday.

The United States has expressed interest in cooperating with India as their spacecraft gather data about the planet.

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A CASE OF ICHCHTHYOSIS ; A TYPICAL SKIN DISORDER ; E.T.G AYURVEDASCAN TEST EVALUATION ; “इक्थियासिस” जैसे लाइलाज चर्म रोग का ई०टी०जी० आयुर्वेदास्कैन आधारित आन्कलन

September 25, 2014 1:03 am / 1 Comment on A CASE OF ICHCHTHYOSIS ; A TYPICAL SKIN DISORDER ; E.T.G AYURVEDASCAN TEST EVALUATION ; “इक्थियासिस” जैसे लाइलाज चर्म रोग का ई०टी०जी० आयुर्वेदास्कैन आधारित आन्कलन

**आधुनिक युग आयुर्वेद ** ई०टी०जी० आयुर्वेदास्कैन ** DIGITAL AYURVEDA TRIDOSHO SCANNER**AYURVED H. T. L. WHOLE-BODY SCANNER**आयुषव्यूज रक्त केमिकल केमेस्ट्री परीक्षण अनालाइजर ** डिजिटल हैनीमेनियन होम्योपैथी स्कैनर **

चर्म रोग ICHCHTHYOSIS या इख्तोयासिस एक तरह की ऐसी तकलीफ है जो त्वचा के टिश्यूज से जुड़ी हुयी बीमारी है / इस बीमारी मे त्वचा का रन्ग काला पड़ जाता है और त्वचा मोटी हो जाती है / इसके अलावा त्वचा का रन्ग काला और वर्ण cracks यानी फटी हुयी और आकार मछली की खाल जैसा हो जाता है /

जिस मरीज का नीचे दिया गया चित्र है उसे लगभग चार साल से यह तकलीफ रही है / अन्ग्रेजी और देशी और होम्योपैथी का इलाज कराने के बाद इसे आराम नही मिला / हमारे यहा से इलाज करा चुके एक मरीज द्वारा हमारे सन्स्थान मे इलाज कराने के लिये प्रोत्साहित किये जाने के बाद यह मरीज इलाज के लिये हमारे यहां आया है /

मरीज के दोनो पैरो और शरीर के लगभग सभी हिस्सो मे इसी तरह के scabs मौजूद है /.

नीचे दिये गये चित्र मे यह चर्म रोग…

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Ibritumomab tiuxetan

September 24, 2014 6:59 am / Leave a comment

Ibritumomab tiuxetan, sold under the trade name Zevalin, is a monoclonal antibody radioimmunotherapy treatment for relapsed or refractory, low grade or transformed B cell non-Hodgkin’s lymphoma, a lymphoproliferative disorder. The drug uses the monoclonal mouse IgG1 antibody ibritumomab (pronounced as <ih bri TYOO mo mab>)^[1] in conjunction with the chelator tiuxetan, to which a radioactive isotope (either yttrium-90 or indium-111) is added. Tiuxetan is a modified version of DTPA whose carbon backbone contains an isothiocyanatobenzyl and a methyl group.^[2]^[3]

Mechanism of action

The antibody binds to the CD20 antigen found on the surface of normal and malignant B cells (but not B cell precursors), allowing radiation from the attached isotope (mostly beta emission) to kill it and some nearby cells. In addition, the antibody itself may trigger cell death via antibody-dependent cell-mediated cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC), and apoptosis. Together, these actions eliminate B cells from the body, allowing a new population of healthy B cells to develop from lymphoid stem cells.

Zevalin (Ibritumomab tiuxetan) is a radio-labeled antibody. The antibody seeks and binds to cells that have a receptor called CD20 — present on both normal and malignant mature b-cells.

Once bound to the target cells, Zevalin delivers radiation, which enhances the killing effect of the antibody.

Because immature b-cells do not have the CD20 receptor, normal b-cells will recover in about nine months after treatment.

Rituxan (the naked antibody) is administered prior to Zevalin with the goal of clearing the majority of normal b-cells so that the therapeutic dose (the radio-labeled antibody) is more focused on tumor cells.

Preparation

Zevalin is supplied as a single dosage kit supplied by IDEC Pharmaceuticals Corp. It consists of Ibritumomab covalently conjugated to the metal chelator tiuxetan, which forms a stable complex with indium-111 for imaging and yttrium-90 for therapy.

The kit is supplied with four vials – a vial containing 3.2 mg of conjugated antibody in 2 ml saline, a vial containing 2 ml 50mM sodium acetate, a vial containing phosphate buffer, and a fourth empty reaction vial. Prior to labeling, a volume of sodium acetate buffer equivalent to 1.2 times the volume of the tracer solution is transferred to the reaction vial. Then 5.5 mCi (203.5 MBq) indium-111 or 40mCi (1.48 GBq) yttrium-90 is added to the reaction vial and mixed thoroughly without shaking. Next, 1.3 ml of conjugated antibody is added. The mixture is incubated for exactly 30min for indium-111 and for 5 min with yttrium-90 labeling, followed by the addition of enough phosphate buffer to make the final volume 10 ml. The labeling yield is determined by ITLC-SG with 0.9% saline as the mobile phase. Labeling efficiency should be greater than 95%.^[4]

http://pubs.rsc.org/en/content/articlelanding/2006/cs/b514859f/unauth#!divAbstract

A cartoon depiction of the radiolabelled monoclonal antibody 90Y-ibritumomab tiuxetan 18.

Administration

In order to qualify for ibritumomab, a patient needs to have bone marrow involvement of < 25% and > 15% bone marrow cellularity. Since ibritumomab is known to cause cytopenia, platelet and neutrophil counts are also taken pretreatment. Refractory/relapsed patients should have platelet counts of 100,000 per cubic millimetre (100,000/cmm) or greater; consolidation patients should have counts of 150,000/cmm or greater. Since a murine antibody is used, the patient might also be tested for human anti mouse antibodies (HAMA). Having bulky disease does not disqualify a patient.

The ibritumomab regimen takes 7–9 days. An imaging dose of the drug is no longer required in the U.S. Rituxan 250 mg/sq.m is given day 1, then on day 7-9 the Rituxan dose is repeated and Zevalin given within four hours. The dose of Zevalin 0.4 m Ci/kg (= 14.8M Bq/kg) if platelet counts are above 150,000/cmm; 0.3 mCi/kg (= 11.1MBq/kg) if 100,000-150,000/cmm. The Zevalin dose never exceeds 32 mCi (= 1184MBq).^[5]

Ibritumomab tiuxetan is administered by intravenous infusion which usually lasts around 10 minutes. Only acrylic shielding is needed, not lead. A trained nuclear medicine technologist performs the infusion and safely disposes of waste.

Efficacy

Treatment with ibritumomab showed higher response rates in clinical trials compared to treatment with only rituximab (similar to ibritumomab, but without the attached radioisotope), and showed very promising results for patients who no longer respond to rituximab.

In patients with relapsed or refractory low-grade, follicular, or transformed B-cell NHL, where no prior anti-CD20 therapy was allowed, the ORR was 83% / 55% and CR was 38% / 18%, comparing ibritumomab to rituximab. ^[6]

Recently, extended follow-up data for the ZEVALIN ([90Y]-ibritumomab tiuxetan) First-line Indolent (FIT) study presented at the American Society of Hematology (ASH) Annual Meeting demonstrated the continued improvement in progression-free survival (PFS) following ibritumomab consolidation therapy for patients with follicular B-cell non-Hodgkin’s lymphoma who achieved a response to first-line therapy over chemotherapy alone. Additionally, ibritumomab consolidation did not adversely affect the use of various effective second-line treatments including stem cell transplants in patients who relapsed.^[7]

In a Phase II study on patients with relapsed and refractory mantle cell lymphoma, the OR was 42% and CR was 26%.^[8]

A study demonstrated that rituximab followed by single agent ibritumomab in a front-line setting for patients with MALT lymphoma and low-grade follicular lymphoma that primarily involved the conjunctiva or orbit, produced a complete response rate of 83 percent.^[9]

http://rd.springer.com/article/10.2165%2F00024669-200201050-00004#page-1

History

Developed by the IDEC Pharmaceuticals, which is now part of Biogen Idec, ibritumomab tiuxetan was the first radioimmunotherapy drug approved by the Food and Drug Administration (FDA) in 2002 to treat cancer. It was approved for the treatment of patients with relapsed or refractory, low‑grade or follicular B‑cell non‑Hodgkin’s lymphoma (NHL), including patients with rituximab refractory follicular NHL.

In December 2007, Cell Therapeutics Inc acquired the U.S. rights to sell, market, and distribute this radioimmunotherapy antibody from Biogen for approximately US$30 million, or the equivalent of about two years’ net sales revenue in the U.S. for the drug.^[10] Outside of the U.S., Bayer Schering Pharma continues to have the rights to the drug.

In March 2009, Spectrum Pharmaceuticals acquired 100% control of RIT Oncology, LLC, to commercialize Zevalin in the US. Now Spectrum Pharmaceuticals is responsible for all activities relating to Zevalin in the US.

In September 2009, ibritumomab received approval from the FDA for an expanded label for the treatment of patients with previously untreated follicular non-Hodgkin’s Lymphoma (NHL), who achieve a partial or complete response to first-line chemotherapy.

Costs

Ibritumomab which is not available in a generic form because it is still under patent protection, is currently the most expensive drug available given in a single dose, costing over US$ 37,000 (€ 30,000) for the average dose. However, ibritumomab is essentially an entire course of lymphoma therapy which is delivered in 7–9 days, with one visit for pre-dosing Rituxan, and one visit a week later for the actual Zevalin therapeutic dose preceded by Rituxan. Compared to other monoclonal antibody treatments (many of which are well over US$ 40,000 for a course of therapy), this drug is priced in the middle for many of these therapies.

Ibritumomab tiuxetan ^?
Monoclonal antibody

Type	Whole antibody
Source	Mouse
Target	CD20
Clinical data
Trade names	Zevalin
AHFS/Drugs.com	monograph
Licence data	US FDA:link
Legal status	US: ℞-only
Routes	intravenous
Identifiers
CAS number	174722-31-7
ATC code	V10XX02 (⁹⁰Y)
DrugBank	DB00078

External links

http://www.fda.gov/ohrms/dockets/ac/01/slides/3782s2_02_idec/sld015.htm

References

Ibritumomab: Pronunciation
Milenic, Diane E.; Brady, Erik D.; Brechbiel, Martin W. (June 2004). “Antibody-targeted radiation cancer therapy”. Nat Rev Drug Discov 3 (6): 488–499. doi:10.1038/nrd1413. ISSN 1474-1776. PMID 15173838.
WHO Drug Information
http://www.accessdata.fda.gov/drugsatfda_docs/label/2002/ibriide021902LB.pdf
Ibritumomab: Indications
Ibritumomab: Efficacy
ZEVALIN Consolidation in First-Line Therapy in Patients with Non-Hodgkin’s Lymphoma Resulted in a Progression-Free Survival of Greater Than 67 Months
Zevalin and mantle cell
ZEVALIN(R) Produced 83 Percent Complete Response Rate in Mucosa-Associated Lymphoid Tissue (MALT) Orbital Lymphoma Study
[1]

// // // // //

September 23, 2014

// CASI Signs China Licensing Deal With Spectrum For 3 Cancer Drugs…http://www.outsourcedpharma.com/doc/casi-signs-china-licensing-deal-with-spectrum-for-cancer-drugs-0001

// CASI Signs China Licensing Deal With Spectrum For 3 Cancer Drugs// // // // //

CASI Pharmaceuticals and Spectrum Pharmaceuticals (SPPI) announced the signing of a license agreement that gives CASI exclusive rights to develop three cancer drugs from Spectrum and market them in China, including Macau, Hong Kong, and Taiwan.

The agreement concerns the two approved cancer drugs Zevalin (ibritumomab tiuxetan) Injection non-Hodgkin’s lymphoma (NHL) and Marqibo (vinCRIStine sulfate LIPOSOME injection) for acute lymphoblastic leukemia (ALL) as well as the investigational Phase 3 drug Captisol-Enabled Melphalan (CE melphalan) being studied as a conditioning treatment before autologous stem cell transplant in patients with multiple myeloma. Spectrum recently reported that Melphalan met its primary endpoint in its pivotal safety and efficacy trial. In view of the results, Spectrum said it intends to file a New Drug Application (NDA) with the U.S. Food and Drug Administration (FDA) for the drug in the second half of 2014.

// // // // //

Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors

September 23, 2014 1:12 pm / Leave a comment

COMPD HAS cas no 1616882-93-9

MF……….C₁₈ H₁₁ F₃ N₂ O₂

[1]Benzopyrano[4,3-c]pyrazol-4(1H)-one, 3-methyl-1-[4-(trifluoromethyl)phenyl]-

3-Methyl-1-(4-(trifluoromethyl)phenylchromeno[4,3-c]pyrazol-4(1H)-one

Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors

Bioorganic & Medicinal Chemistry Letters,Volume 24, Issue 19, 1 October 2014, Pages 4638–4642

DOI: 10.1016/j.bmcl.2014.08.050

Jagdeep Grover, Vivek Kumar, M. Elizabeth Sobhia, Sanjay M. Jachak

http://www.sciencedirect.com/science/article/pii/S0960894X14008944

Abstract

As a part of our continued efforts to discover new COX inhibitors, a series of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones were synthesized and evaluated for in vitro COX inhibitory potential. Within this series, seven compounds (3a–d, 3h, 3k and 3q) were identified as potential and selective COX-2 inhibitors (COX-2 IC₅₀’s in 1.79–4.35 μM range; COX-2 selectivity index (SI) = 6.8–16.7 range). Compound 3b emerged as most potent (COX-2 IC₅₀ = 1.79 μM; COX-1 IC₅₀ >30 μM) and selective COX-2 inhibitor (SI >16.7). Further, compound 3b displayed superior anti-inflammatory activity (59.86% inhibition of edema at 5 h) in comparison to celecoxib (51.44% inhibition of edema at 5 h) in carrageenan-induced rat paw edema assay. Structure–activity relationship studies suggested that N-phenyl ring substituted with p-CF₃ substituent (3b, 3k and 3q) leads to more selective inhibition of COX-2. To corroborate obtained experimental biological data, molecular docking study was carried out which revealed that compound 3b showed stronger binding interaction with COX-2 as compared to COX-1.

Authors

^a Department of Natural Products, National Institute of Pharmaceutical Education and Research, Sector-67, S.A.S. Nagar (Mohali) 160062, Punjab, India
^b Department of Pharmacoinformatics, National Institute of Pharmaceutical Education and Research, Sector-67, S.A.S. Nagar 160062, Punjab, India

Sanjay Corresponding author. Tel.: +91 172 2214683; fax: +91 172 2214692.

CLICK……….

Supplementary data

Cyclooxygenase (COX) or prostaglandin endoperoxide synthase (PGHS), catalyzes the conversion of arachidonic acid to inflammatory mediators such as prostaglandins (PGs), prostacyclins and thromboxanes. COX exists in mainly two isoforms: COX-1 and COX-2. Nonsteroidal anti-inflammatory drugs (NSAIDs), widely used for relief of fever, pain and inflammation, act by inhibiting COX catalyzed biosynthesis of inflammatory mediators.

However, the therapeutic use of classical NSAIDs is associated with well-known side effects at the gastrointestinal level (mucosal damage, bleeding) and, less frequently, at the renal level.

Two decades after the discovery of COX isoforms, it was recognized that selective inhibition of COX-2 might be endowed with improved anti-inflammatory properties and reduced gastrointestinal toxicity profiles than classical NSAIDs.

Overall, these selective COX-2 inhibitors (coxibs) have fulfilled the hope of possessing reduced risk in gastrointestinal events, but unfortunately cardiovascular concerns regarding the use of these agents have emerged that led to the withdrawal of rofecoxib (Vioxx) and valdecoxib (Bextra) from the market in 2004 and 2005, respectively.

Ongoing safety concerns pertaining to the use of non-selective NSAIDs have spurred development of coxibs with improved safety profile.

……………………………………………………………………………………………..

cas no 1616882-93-9

mf……….C₁₈ H₁₁ F₃ N₂ O₂

[1]Benzopyrano[4,3-c]pyrazol-4(1H)-one, 3-methyl-1-[4-(trifluoromethyl)phenyl]-

3-Methyl-1-(4-(trifluoromethyl)phenylchromeno[4,3-c]pyrazol-4(1H)-one

Scheme 1.

Reagent and conditions: (a) Piperidine, rt, 20 min; (b) ArNHNH₂, EtOH, reflux, 5 h; (c) K₂CO₃, acetone, reflux, 24 h.

COMPD IS

R1=H

R2= H

4-CF₃-C₆H₄

3-Methyl-1-(4-(trifluoromethyl)phenylchromeno[4,3-c]pyrazol-4(1H)-one (3b):

White solid; yield 90%; mp: 224–225 °C;

1H NMR (CDCl3, 400 MHz): δ ppm 7.89 (d, 2H, J = 8.32 Hz, Ar-H), 7.73 (d, 2H, J = 8.24 Hz, Ar-H), 7.45–7.52 (m, 2H, H-6, H-7), 7.16 (dd, 1H, J = 1.4, 8.2 Hz, H-9), 7.10 (td, 1H, J = 1.56, 7.38 Hz, H-8), 2.69 (s, 3H, CH3);

13C NMR (CDCl3, 100 MHz): δ ppm 157.7, 153.3, 151.5, 142.3, 141.8, 131.9, 127.2, 127.1, 127.0, 124.0, 122.2, 118.3, 111.5, 107.1, 12.8;

HRMS (ESI) m/z: Calcd for C18H11F3N2O2Na [M + Na]+ 367.0670; found 367.0676.

Synthetic Communications (2014), 44(13), 1914-1923

DOI:: 10.1080/00397911.2013.879184

Jagdeep Grover^a, Somendu Kumar Roy^a & Sanjay Madhukar Jachak^a^*

pages 1914-1923

http://www.tandfonline.com/doi/abs/10.1080/00397911.2013.879184#.VCI5f0DgXXM

http://www.tandfonline.com/doi/suppl/10.1080/00397911.2013.879184/suppl_file/lsyc_a_879184_sm8537.pdf

Abstract

Unprecedented cyclization was observed during N-sulfonylation of 3-[1-(phenylhydrazono)-ethyl]-chromen-2-one in pyridine, affording 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones. To avoid use of noxious pyridine, reaction was tried in different basic conditions and the best results were obtained with potassium carbonate in acetone. A wide range of substrates bearing either electron-donating or electron-withdrawing substituents on phenylhydrazine ring were compatible with the developed methodology. Rapid access of starting material, 3-acetylcoumarin, excellent yields of products, and use of environmentally benign base and solvent for the cyclization make this strategy an efficient and convenient method for synthesis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones.

Methyl-1-(4-(trifluoromethyl)phenylchromeno[4,3-c]pyrazol-4(1H)-one (4b):

Whitesolid;

yield 90%; mp: 224–225 °C;

1H NMR (CDCl3, 400 MHz):δppm 2.69 (s, 3H, CH3),

7.10(td, 1H,J= 1.56, 7.38 Hz, H-8),

7.16 (dd, 1H,J= 1.4, 8.2 Hz, H-9),

7.45–7.52 (m, 2H, H-6, H-7),

7.73 (d, 2H,J= 8.24 Hz, Ar-H),

7.89 (d, 2H,J= 8.32 Hz, Ar-H);

13C NMR (CDCl3, 100MHz):

δppm 12.8, 107.1, 111.5, 118.3, 122.2, 124.0,

127.0, 127.1, 127.2, 131.9, 141.8, 142.3,

151.5, 153.3, 157.7;

HRMS (ESI)m/z: Calcd for C18H11F3N2O2Na [M + Na]+367.0670; found367.0676.

3-Methyl-1-(4-(trifluoromethyl)phenylchromeno[4,3-c]pyrazol-4(1H)-one

SEE BELOW 1H NMR, 13CNMR, AND MASS SPEC

References
1. Jones, G.; Willett, P.; Glen, R. C.; Leach, A. R.; Taylor, R. J. Mol. Biol. 1997, 267, 727.
2. Bernstein, F. C.; Koetzle, T. F.; Williams, G. J. B.; Meyer, E. F.; Brice, M. D.; Rodgers, J. R.; Kennard, O.; Shimanouchi, T.; Tasumi, M. J. Mol. Biol. 1977, 112, 535.

Selective inhibitors of the Janus kinase Jak3—Are they effective?

September 23, 2014 1:06 pm / Leave a comment

Full-size image (30 K)

Selective inhibitors of the Janus kinase Jak3—Are they effective?

Bioorganic & Medicinal Chemistry Letters

Volume 24, Issue 19, 1 October 2014, Pages 4617–4621

DOI: 10.1016/j.bmcl.2014.08.046

http://www.sciencedirect.com/science/article/pii/S0960894X14008907

Abstract

Jak3, together with Jak1, is involved in signal transduction initiated by cytokines signaling through the common gamma chain which are important in immune homeostasis and immune pathologies. Based on genetic evidence Jak3 has been considered to be an attractive target for immunosuppression. The Jak inhibitor tofacitinib (CP-690,550) which is an approved drug for rheumatoid arthritis was originally introduced as a selective Jak3 inhibitor, however, it also inhibits Jak1 and Jak2. The search for new selective Jak3 inhibitors has yielded several compounds whose profiles will be reviewed here. Implications on Jak3 as a therapeutic target are also discussed.

notes

JAnus Kinase 3 (JAK3) is a member of the JAK family of non-receptor protein tyrosine kinases (PTKs) that include the closely related isoforms—namely, JAK1, JAK2 and tyrosine kinase 2 (TYK2). The realization that human defects in JAK3 signaling result in the clinical manifestation of a severe combined immunodeficiency (SCID) phenotype has suggested that selective JAK3 inhibitors may be useful as therapeutic agents in the areas of organ transplantation and autoimmune diseases. In addition, the promising clinical efficacy reported for the JAK3 inhibitor CP-690,550 in rheumatoid arthritis patients is noteworthy and suggests that obtaining efficacy comparable to, or perhaps better than, the current marketed biologic therapies in this disease may be possible with a small molecule. Although the highly selective inhibition of JAK3 for immunosuppression is particularly attractive from a safety perspective, it remains to be convincingly demonstrated in the clinic. While CP-690,550 does potently inhibit JAK3, it has been shown to inhibit to some extent other JAK family members—namely, JAK1 and JAK2, which may contribute to enhance efficacy in the clinic relative to purely selective JAK3 inhibition.

Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm

September 23, 2014 8:26 am / Leave a comment

LY 3000328

Eli Lilly….INNOVATOR

(3R,4S)-4-(4-fluorobenzamido)-6-(4-(oxetan-3-yl)piperazin-1-yl methylcarbamate

Specific rotation: [α]D25 = 55.19 (c = 10,DMSO).

Cathepsin S (Cat S) plays an important role in many pathological conditions, including abdominal aortic aneurysm (AAA). Inhibition of Cat S may provide a new treatment for AAA. To date, several classes of Cat S inhibitors have been reported, many of which form covalent interactions with the active site Cys25. Herein, we report the discovery of a novel series of noncovalent inhibitors of Cat S through a medium-throughput focused cassette screen and the optimization of the resulting hits. Structure-based optimization efforts led to Cat S inhibitors such as 5 and 9 with greatly improved potency and drug disposition properties. This series of compounds binds to the S2 and S3 subsites without interacting with the active site Cys25.

On the basis of in vitro potency, selectivity, and efficacy in a CaCl2-induced AAA in vivo model, 5(LY3000328) was selected for clinical development.

Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm
http://pubs.acs.org/doi/full/10.1021/ml500283g

Prabhakar K. Jadhav ^*,et al

Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, United States

ACS Med. Chem. Lett., Article ASAP

DOI: 10.1021/ml500283g

Publication Date (Web): August 27, 2014

see

http://pubs.acs.org/doi/suppl/10.1021/ml500283g/suppl_file/ml500283g_si_001.pdf

Abdominal aortic aneurysm
Classification and external resources
CT reconstruction image of an abdominal aortic aneurysm

Abdominal aortic aneurysm (also known as AAA,^[1] pronounced “triple-a”) is a localized dilatation (ballooning) of the abdominal aortaexceeding the normal diameter by more than 50 percent, and is the most common form of aortic aneurysm. Approximately 90 percent of abdominal aortic aneurysms occur infrarenally (below the kidneys), but they can also occur pararenally (at the level of the kidneys) orsuprarenally (above the kidneys). Such aneurysms can extend to include one or both of the iliac arteries in the pelvis.

Abdominal aortic aneurysms occur most commonly in individuals between 65 and 75 years old and are more common among men and smokers. They tend to cause no symptoms, although occasionally they cause pain in the abdomen and back (due to pressure on surrounding tissues) or in the legs (due to disturbed blood flow). The major complication of abdominal aortic aneurysms is rupture, which is life-threatening, as large amounts of blood spill into the abdominal cavity, and can lead to death within minutes.^[2] Mortality of rupture repair in the hospital is 60% to 90%.

Treatment is usually recommended when an AAA grows to >5.5 cm in diameter. While in the past the only option for the treatment of AAA was open surgery, today most are treated with Endovascular Aneurysm Repair (EVAR).^[3] EVAR has been widely adopted, as EVAR has a lower risk of death associated with surgery (0.5% for EVAR vs 3% for open surgery).^[4] Open surgery is sometimes still preferred to EVAR, as EVAR requires long-term surveillance with CT Scans.^[5]

There is moderate evidence to support screening in individuals with risk factors for abdominal aortic aneurysms (e.g., males ≥65).

DATA

HPLC purity = 98.6% (tR = 24.2 min) by HPLC method 3. ee = 99.9% (tR = 23.6 min) by Chiral HPLC method 4.

Specific rotation: [α]D25 = +55.19 (c = 10,DMSO).

1H NMR (400 MHz, DMSO-d6) δ 8.92 (d, J = 7.8 Hz, 1H), 8.01 – 7.90 (m, 2H), 7.34 –
7.23 (m, 2H), 7.19 (q, J = 4.5 Hz, 1H), 6.87 (dd, J = 9.0, 2.9 Hz, 1H), 6.78 – 6.69 (m, 2H), 5.03
(dd, J = 8.1, 3.7 Hz, 1H), 4.86 (td, J = 4.1, 1.8 Hz, 1H), 4.52 (t, J = 6.5 Hz, 2H), 4.41 (t, J = 6.0
Hz, 2H), 4.23 (dd, J = 11.8, 1.9 Hz, 1H), 4.13 (ddd, J = 11.8, 4.4, 1.6 Hz, 1H), 3.39 (p, J = 6.3
Hz, 1H), 2.96 (t, J = 4.9 Hz, 4H), 2.52 (d, J = 4.5 Hz, 3H), 2.34 (t, J = 4.9 Hz, 4H).

13C NMR (DMSO-d6, 100 MHz): δ 165.4, 164.5 (d, J = 248.7 Hz), 156.1, 148.2, 146.2, 131.0, 130.8 (d, J =
9.5 Hz), 120.9, 118.6, 117.6, 117.2, 115.6 (d, J = 21.3 Hz), 74.8, 68.7, 64.3, 58.9, 49.8, 49.5,
47.7, 27.4.

HRMS (ESI+): calcd. for C25H30FN4O5 (M+1): 485.2195, found 485.2188.

1H nmr LY3000328

13 C nmr LY3000328

Logan, Carolynn M.; Rice, M. Katherine (1987). Logan’s Medical and Scientific Abbreviations. Philadelphia: J. B. Lippincott Company. p. 3. ISBN 0-397-54589-4.
Upchurch GR, Schaub TA (2006). “Abdominal aortic aneurysm”. Am Fam Physician 73(7): 1198–204. PMID 16623206.
Chadi SA et al (2012). “Trends in management of abdominal aortic aneurysms”. J Vasc Surg 55 (4): 924–8. doi:10.1016/j.jvs.2011.10.094. PMID 22226189.
Lederle FA, Freishlag JA et al (209). “Outcomes Following Endovascular vs Open Repair of Abdominal Aortic Aneurysm: A Randomized Trial”. JAMA 302 (14): 1535–42.doi:10.1001/jama.2009.1426. PMID 19826022.
Kirkpatrick VE et al (Dec 2013). “Surveillance Computed Tomographic Arteriogram (CTA) Does Not Change Management before Three Years in Patients Who Have a Normal Post-EVAR Study”. Ann Vasc Surg 28 (4): 831–6. doi:10.1016/j.avsg.2013.09.017.PMID 24361383

Keywords:

Cathepsin, abdominal aortic aneurysm, development candidate, noncovalent, Cathepsin S Inhibitor, LY3000328,

EU OK’s Gilead’s rare blood cancers drug

September 22, 2014 4:41 am / Leave a comment

EU OK's Gilead's rare blood cancers drug

SEPT 21 , 2014

Patients with the incurable blood cancers chronic lymphocytic leukaemia (CLL) and follicular lymphoma (FL) have gained access to a new treatment option in Europe with the approval of Gilead’s Zydelig (idelalisib).

For CLL, the drug can now be used alongside Rituxan (rituximab) in patients who have received at least one prior therapy, and it has also been green lighted for first-line use in those carrying a 17p deletion or TP53 mutation who are unsuitable for chemo-immunotherapy.

SEE

SYNTHESIS AT

https://newdrugapprovals.org/2014/01/14/idelalisib-us-fda-accepts-nda-for-gileads-idelalisib-for-the-treatment-of-refractory-indolent-non-hodgkins-lymphoma/

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Costs

External links

References

September 23, 2014

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Abstract

Abstract

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Abstract

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Keywords:

Cathepsin, abdominal aortic aneurysm, development candidate, noncovalent, Cathepsin S Inhibitor, LY3000328,

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