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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Novartis Japan Achieves Primary Endpoint In HER2 Positive Advanced Breast Cancer Phase III Afinitor Trials
Everolimus
Novartis announced it achieved its primary endpoint of significantly extending progression-free survival with Afinitor (everolimus) in Phase III trials of patients with HER2 positive advanced breast cancer.
read all at
Everolimus (RAD-001) is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an inhibitor of mammalian target of rapamycin (mTOR).
It is currently used as an immunosuppressant to prevent rejection of organ transplants and treatment of renal cell cancer and other tumours. Much research has also been conducted on everolimus and other mTOR inhibitors for use in a number of cancers.
It is marketed by Novartis under the tradenames Zortress (USA) and Certican (Europe and other countries) in transplantation medicine, and Afinitor in oncology.
Daiichi Sankyo enrolls first patient in Nimotuzumab Phase 3 clinical trials
Nimotuzumab
25 April 2013
Daiichi Sankyo Company, Limited announced today that the first patient has been enrolled in two pivotal phase 3 clinical trials of nimotuzumab (DE-766), a recombinant humanized monoclonal antibody targeting the Epidermal Growth Factor Receptor (EGFR), which is being evaluated for the treatment of patients diagnosed with lung cancer and with gastric cancer.
About Phase 3 Clinical Trials for Lung Cancer
The phase 3 clinical trial is a multicenter, randomized, double-blind, placebo-controlled study investigating nimotuzumab for the first-line therapy in patients with unresectable and locally advanced squamous cell lung cancer. The patients will receive either nimotuzumab in combination with concurrent chemoradiotherapy or placebo in combination with concurrent chemoradiotherapy. The primary endpoint is overall survival (OS), and the secondary endpoints are progression free survival (PFS) and safety. Approximately 420 patients are planned to be enrolled at approximately 60 clinical centers in Japan. Additional details of the trial are available onwww.clinicaltrials.jp/user/cteSearch.jsp.
About Phase 3 Clinical Trials for Gastric Cancer (ENRICH study)
The ENRICH study is a randomized, open-label, Japan-Korea collaborative study of previously treated patients with EGFR overexpressed advanced gastric and gastroesophageal junction cancer who will receive either nimotuzumab and irinotecan hydrochloride hydrate (hereafter, irinotecan) combination therapy or irinotecan monotherapy. The primary endpoint is overall survival (OS), and the secondary endpoints are progression free survival (PFS) and safety. Approximately 400 patients are planned to be enrolled at approximately 40 clinical centers in Japan and South Korea. In Korea, Kuhnil Pharmaceutical Company, Limited (hereafter, Kuhnil) is implementing this trial. Additional details of the trial are available on www.clinicaltrials.gov.
About Unresectable and Locally Advanced Squamous Cell Lung Cancer
In Japan, lung cancer is the first leading cause of cancer death, with about 70,000 deaths in 2011.i Non-small cell lung cancer (adenocarcinoma, squamous cell carcinoma, and large cell carcinoma) occupies more than 80 percent of lung cancer. Concurrent chemoradiotherapy for a radical cure is currently used as the standard treatment for patients with stage III locally advanced non-small cell lung cancer, in which radical surgery is not possible but radiotherapy is.ii Of these cases, between 30 and 40 percent are squamous cell carcinoma and EGFR is known to be overexpressed.iii
About Gastric Cancer
Half of the total number of gastric cancer cases worldwide occurs in Eastern Asia.iv In Japan, gastric cancer is the second leading cause of cancer death, with an estimated about 50,000 deaths. i In South Korea, about 10,000 gastric cancer deaths in 2011 were reported.v Numerous improvements have occurred in the management of gastric cancer; however, gastric cancer still has a poor prognosis. For patients with earlier stages of disease, more than 50% undergo surgery, but even after a curative resection, 60% of these patients eventually relapse locally or with distant metastases. vi
About Nimotuzumab and EGFR
Nimotuzumab is an intravenously administered recombinant humanized monoclonal antibody directed against human EGFR and is produced by CIMAB S.A. (Cuba). Nimotuzumab blocks the binding of EGF to its receptor interfering with the cell signaling pathway. Nimotuzumab has been approved for head and neck cancer, glioma, and esophageal cancer in several countries. EGFR is known to be overexpressed in a wide variety of human tumors.vii Overexpression of EGFR in tumors correlates with increased metastasis, decreased survival, and a poor prognosis. It is known that EGFR is activated by exposure to radiation.
In 2006, Daiichi Sankyo introduced nimotuzumab from CIMAB S.A. and CIMYM BioSciences Inc. (Canada) and has the rights to develop and commercialize in Japan. In Korea, Kuhnil has the rights to develop and commercialize.
MHLW Japan, GlaxoSmithKline and Genmab announced the approval of Arzerra (ofatumumab) by the MHLW for use in patients with relapsed/refractory CD20-positive chronic lymphocytic leukaemia.
mar 26, 2013
GlaxoSmithKline and Genmab announced the approval of Arzerra (ofatumumab) by the MHLW for use in patients with relapsed/refractory CD20-positive chronic lymphocytic leukaemia.
The thumbs-up triggers a milestone payment of 20 million Danish kroner to Genmab.
Ofatumumab(trade name Arzerra, also known as HuMax-CD20) is a human monoclonal antibody (for the CD20 protein) which appears to inhibit early-stage B lymphocyte activation. It is FDA approved for treating chronic lymphocytic leukemia that is refractory to fludarabine and alemtuzumab (Campath) and has also shown potential in treating Follicular non-Hodgkin’s lymphoma, Diffuse large B cell lymphoma, rheumatoid arthritis and relapsing remitting multiple sclerosis. Ofatumumab has also received conditional approval in Europe for the treatment of refractory chronic lymphocytic leukemia. This makes ofatumumab the first marketing application for an antibody produced by Genmab, as well as the first human monoclonal antibody which targets the CD20 molecule that will be available for patients with refractory CLL.
Nippon and Teva receive approval for biosimilar G-CSF (fligrastim) in Japan
As with the original drug, acts on neutrophil precursor cells, to promote the proliferation, differentiation and its biosimilar filgrastim of (recombinant) promotes the release of neutrophils from the bone marrow, enhances its function. In the field of cancer treatment, it is used for chemotherapy-induced neutropenia mainly cancer.
Filgrastim is a granulocyte colony-stimulating factor (G-CSF) analog used to stimulate the proliferation and differentiation of granulocytes.[1] It is produced by recombinant DNA technology. The gene for human granulocyte colony-stimulating factor is inserted into the genetic material of Escherichia coli. The G-CSF then produced by E. coli is different from G-CSF naturally made in humans.
It is marketed by Amgen under the brand name Neupogen, in India it is also marketed by Abbott Healthcare under the brand name Imumax, Dr. Reddy’s Laboratories under the brand name Grafeel, In Pakistan CCL Pharmaceuticals (Pvt) Ltd under the brand name Grastin, Zenotech Laboratories Limited under the brand name Nugraf, Raichem lifesciences under the brand name Shilgrast, Intas Biopharmaceuticals under the brand name Neukine, Emcure biopharmaceuticals under the brand name Emgrast, Reliance Life Sciences under the brand name Religrast and Sandoz under the name Zarzio.
Apricus Biosciences is currently developing and testing a product (under the brand name Nupen) which can deliver filgrastim through the skin to improve post-chemotherapy recovery of neutrophil counts.
Phase 2 SMP-986(afacifenacin fumarate) Overactive bladder/ Dainippon Sumitomo Pharma and Nippon Shinyaku conclude a license agreement for SMP-986, a therapeutic agent for urology
877606-63-8 cas no of afacifenacin
any str error, mail to amcrasto@gmail.com
SMP-986 (afacifenacin fumarate)
(4S)-4-phenyl-3-(1-{[3-(trifluoromethoxy)phenyl]methyl}piperidin- 4-yl)-3,4-dihydroquinazolin-2(1H)-one muscarinic receptor antagonist
- Developed in-house
- SMP-986 possesses the dual pharmacological actions of muscarinic receptor antagonism (non-selective) and inhibition of the bladder afferent pathway through Na+-channel blockade. This compound is being evaluated for its ability to ease urinary urgency and reduce the frequency of both urination and incontinence. The compound has also exhibited the potential to have lower incidence of side effects related to muscarinic receptor antagonism, such as dry mouth.
- Development stage: Phase II in the U.S. and Europe. Phase II in Japan
7 mar 2013
Dainippon Sumitomo Pharma Co., Ltd. (DSP) and Nippon Shinyaku Co., Ltd. Announce they have concluded a license agreement for exclusive rights to develop, manufacture and commercialize SMP-986 in Japan, a new therapeutic agent for overactive bladder created by DSP.
Taiho Pharma seeks Japanese nod to manufacture,market novel anti-tumour agent TAS-102
TRIFLURIDINE
TIPIRACIL
TAS-102 is an anti-cancer drug under development for colorectal cancer.[1]
| Combination of | |
|---|---|
| Trifluridine | cytotoxin |
| Tipiracil | thymidine phosphorylase inhibitor |
Clinical trials
A phase II trial reported in 2011[2] and a phase III trial is due to end in 2014.[1][3]
Mechanism
TAS-102 consists of the cytotoxin trifluridine and the thymidine phosphorylase inhibitor (TPI) tipiracil.[4] Trifluridine is incorporated into DNA during DNA synthesis and inhibits tumor cell growth. Tipiracil protects trifluridine from being broken down when taken orally.
| February 28, 2013, |
|
Taiho Pharmaceutical Co., Ltd. has submitted an application to the Japanese Ministry of Health, Labour and Welfare for approval of the manufacture and marketing of the novel oral nucleoside anti-tumour agent TAS-102 (combination of trifluorothymidine [FTD] and tipiracil hydrochloride [TPI]). Taiho is seeking approval of TAS-102 for the indication of unresectable, advanced, recurrent colorectal cancer. The application for approval is based on the results of a phase II clinical trial (Study 10040030) conducted at 20 facilities throughout Japan. It was a randomized, double-blind comparative study of TAS-102 and a placebo involving 172 patients with unresectable, advanced, recurrent colorectal cancer that was refractory to the standard chemotherapy of at least two or more regimens containing fluoropyrimidine, irinotecan, and oxaliplatin. The results indicated that the group administered TAS-102 had improved overall survival rates (median overall survival: 9.0 months vs. 6.6 months) and a significantly reduced risk of mortality (HR: 0.56, p=0.0011). The most frequently reported adverse drug reaction with a CTCAE grade of 3 or higher was neutropenia. Grade 3 or higher diarrhea, fatigue, nausea, and other adverse reactions were no more than 10 per cent. Taiho Pharmaceutical is currently proceeding with a global phase III clinical trial of TAS-102 in a similar colorectal cancer population (RECOURSE) with the ultimate goal of global registration and commercialization of the agent. Taiho Pharmaceutical believes that TAS-102 will make a significant contribution to cancer patients and will continue its development efforts to broaden its use. TAS-102 is an anti-tumour agent composed of a combination of trifluorothymidine (FTD), a nucleoside that incorporates into DNA and inhibits a variety of genetic functions required for the proliferation of cancer cells, and tipiracil hydrochloride (TPI), an inhibitor of thymidine phosphorylase (which degrades FTD) that maintains an effective blood concentration of FTD. TAS-102 is administered twice daily to achieve a total daily dose of 70mg/m2 for five days followed by two days of rest and then repeated a second time. This is followed by a 14-day rest period to make a 28-day schedule for one course. |
- “New Drug for Colorectal Cancer Shows Promise in Phase II Trial”. 28 Aug 2012.
- “Novel Drug TAS-102 Makes Headway in Refractory Colorectal Cancer”. 4 Oct 2011.
- “Phase II study of TAS-102 for pretreated metastatic colorectal cancer”. 29 Aug 2012.
- “A novel combination antimetabolite, TAS-102, exhibits antitumor activity in FU-resistant human cancer cells through a mechanism involving FTD incorporation in DNA.”. Sept 2004.
|
|
|---|---|
| TRIFLURIDINE | |
| 1-[4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5- (trifluoromethyl) pyrimidine-2,4-dione |
Trifluridine (also called trifluorothymidine or TFT) is an anti-herpesvirus antiviral drug, used primarily on the eye. It was sold under the trade name, Viroptic, by Glaxo Wellcome, now merged into GlaxoSmithKline. The brand is now owned by Monarch Pharmaceuticals, which is wholly owned by King Pharmaceuticals.
It is a nucleoside analogue, a modified form of deoxyuridine, similar enough to be incorporated into viral DNA replication, but the -CF3 group added to the uracil component blocks base pairing.
It is a component of the experimental anti-cancer drug TAS-102.
TIPIRACIL
| NAME | 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]pyrimidine-2,4-(1H,3H)-dione | |||
| CAS | 183204-74-2 | |||
| MOL F | C9H11ClN4O2 | |||
| STR | |
|||
| USE | potentiator of antineoplastics; | |||
Taiho Pharmaceutical, a subsidiary of Otsuka Holdings Co., Ltd., is an R&D-driven specialty pharma focusing on the three fields of oncology, allergies and immunology, and urology.
New Drug Approvals 