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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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DR ANTHONY MELVIN CRASTO Ph.D

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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Lupin Launches its Oral Contraceptive Daysee™ Tablets in the US Market; Generic of Seasonique® Tablets


MUMBAI, India and BALTIMORE, April 12, 2013

Pharma major, Lupin Ltd., announced today that its subsidiary Lupin Pharmaceuticals Inc. (collectively Lupin) has received final approval for its Daysee Tablets (Levonorgestrel and Ethinyl Estradiol Tablets, USP, 0.15 mg/0.03 mg and Ethinyl Estradiol Tablets, USP, 0.01 mg) from the United States Food and Drugs Administration (US FDA) to market a generic version of Teva Branded Pharm.’s Seasonique Tablets®. Lupin has already commenced shipping the product.

Lupin’s Daysee Tablets is indicated for use by women to prevent pregnancy.

Lupin’s Daysee Tablet (Levonorgestrel and Ethinyl estradiol tablets USP 0.15 mg/0.03 mg and Ethinyl estradiol tablets USP 0.01 mg) is available in Extended-Cycle Wallets each containing a 13-week supply of tablets: 84 light blue tablets, each containing 0.15 mg of Levonorgestrel and 0.03 mg of Ethinyl estradiol, and 7 mustard tablets, each containing 0.01 mg of Ethinyl estradiol. The light blue tablets are round, biconvex, film-coated tablets, debossed with “LU” on one side and “V21” on the other side. The mustard tablets are round, biconvex, film-coated tablets debossed with “LU” on one side and “V22” on the other side.

The total sales for Branded and generic sales for the product stood at USD 161 million (IMS MAT Dec 2012).

About Lupin Limited

Headquartered in Mumbai, Lupin is an innovation led transnational pharmaceutical company producing and developing a wide range of branded and generic formulations and APIs. The Company is a significant player in the Cardiovascular, Diabetology, Asthma, Pediatric, CNS, GI, Anti-Infective and NSAID space and holds global leadership positions in the Anti-TB and Cephalosporin segment.

Lupin is the 5th largest and fastest growing generics player in the US (5.1% market share by prescriptions, IMS Health) and the 3rd largest Indian pharmaceutical company by sales. The Company is also the fastest growing top 10 generic pharmaceutical players in Japan and South Africa (IMS).

For the financial year ended March 2012, Lupin’s Consolidated Total Income and Profit after Tax were Rs. 70,972 million (USD 1.49 billion) and Rs.8,676 million (USD 182 million) respectively. Please visit http://www.lupinworld.com for more information.

Lupin Pharmaceuticals, Inc. is the wholly owned U.S. subsidiary of Lupin Limited.  Headquartered in Baltimore, Maryland, Lupin Pharmaceuticals, Inc. is dedicated to delivering high-quality, affordable generic medicines and branded formulations trusted by healthcare professionals and patients across geographies. For more information, visit http://www.lupinpharmaceuticals.com.

Fostamatinib


vsprasada's avatarMed.Chem.Cool

AstraZeneca Reports Mixed Phase III Results For Rheumatoid Arthritis Candidate

4/5/2013 3:39 AM ET

Anglo-Swedish drug maker AstraZeneca Plc, on Friday said that a phase III study to assess the efficacy and safety of its drug candidate Fostamatinib for rheumatoid arthritis met one primary endpoint, while it failed in its second primary goal.

The trial, dubbed OSKIRA-1, had two primary endpoints namely, assessing signs and symptoms of rheumatoid arthritis as measured by ACR20 response rates, and an X-ray endpoint known as mTSS (modified Total Sharp Score). While Fostamatinib achieved a statistically significant improvement in ACR20 response rate compared to placebo in the trial, it failed to achieve statistical significance in mTSS.

The company added that the safety and tolerability findings for Fostamatinib observed in the OSKIRA-1 study were generally consistent with those previously reported for the TASKi Phase II program. In the study, the most commonly reported adverse events were…

View original post 196 more words

Sorbent begins CLP-1001 Phase 2b trial in heart failure patients


APRIL 2013

Sorbent Therapeutics has begun Phase 2b trial evaluating the safety and efficacy of CLP-1001 in treating signs and symptoms of fluid overload in heart failure patients.

Non-absorbed oral polymer CLP-1001 binds to and removes excess sodium and fluid in the GI tract independently of the kidneys……………read original article at pharmaceutical business review

http://clinicaltrials.pharmaceutical-business-review.com/news/sorbent-begins-clp-1001-phase-2b-trial-in-heart-failure-patients-120413

EMA reviews new Sanofi flu vaccine


EMA reviews new Sanofi flu vaccine

April 12, 2013

 

Sanofi says that regulators in Europe have started to evaluate its four-in-one influenza vaccine.

The French drugmaker’s Sanofi Pasteur unit announced that a decentralised marketing authorisation application has been accepted for review in the European Union for a quadrivalent formulation of its three-strain seasonal influenza vaccine Vaxigrip. France will act as the reference member state.

Currently-licensed vaccines are trivalent and are formulated every year, based on seasonal recommendations made by the World Health Organisation and national authorities. They contain inactivated strains that confer protection against two influenza A virus subtypes and one type B virus.

However, for over a decade, two distinct influenza B families have co-circulated, Sanofi noted, making it difficult to predict which B-lineage strain will predominate in a country or in a region in seasons to come. The new vaccine includes two A and two B strains corresponding to both of the aforementioned B lineages.

Olivier Charmeil, Sanofi Pasteur’s chief executive, said the inclusion of the four flu viruses anticipated to circulate in the forthcoming season “has the potential to reduce the risk of influenza disease and influenza-related complications, specifically hospitalisations and deaths among those, at risk, who contract the disease”.

In October 2012, a supplemental Biologics License Application was filed in the USA for a quadrivalent formulation of Sanofi’s Fluzone vaccine. An action date is anticipated in the second quarter of 2013.

Earlier this month, rival GlaxoSmithKline’s quadrivalent seasonal influenza vaccine, Influsplit Tetra/Fluarix Tetra, was granted marketing authorisation in Germany and the UK, the first four-strain flu jab to be approved in Europe.

Newzealand’s PHARMAC is seeking feedback on a proposal to list pegfilgrastim (Neulastim) and tocilizumab (Actemra) , from 1 July 2013, with Roche Products (NZ) Limited.


https://i0.wp.com/www.voxy.co.nz/files/imagecache/news_item_image/files/pharmac_22.jpg

NEWZEALAND

Tocilizumab and pegfilgrastim

12 April 2013

PHARMAC is seeking feedback on a proposal to list pegfilgrastim (Neulastim) for prevention of neutropenia in patients undergoing cancer chemotherapy, and tocilizumab (Actemra) for systemic juvenile idiopathic arthritis, from 1 July 2013, through a provisional agreement with Roche Products (NZ) Limited.

Feedback sought

PHARMAC welcomes feedback on this proposal. To provide feedback, please submit it in writing by 5:00 pm on Monday 29 April 2013 to:

Geraldine MacGibbon
Senior Therapeutic Group Manager

Email: geraldine.macgibbon@pharmac.govt.nz

Fax: 04 460 4995

Post: PO Box 10 254, Wellington 6143.

All feedback received before the closing date will be considered by PHARMAC’s Board (or Chief Executive acting under delegated authority) prior to making a decision on this proposal.

http://www.pharmac.health.nz/news/item/tocilizumab-and-pegfilgrastim

 

Tocilizumab (INN, or atlizumab, developed by Hoffmann–La Roche and Chugai and sold under the trade names Actemra and RoActemra) is an immunosuppressive drug, mainly for the treatment of rheumatoid arthritis (RA) and systemic juvenile idiopathic arthritis, a severe form of RA in children. It is a humanized monoclonal antibody against the interleukin-6 receptor (IL-6R). Interleukin 6 (IL-6) is a cytokine that plays an important role in immune response and is implicated in the pathogenesis of many diseases, such as autoimmune diseases, multiple myeloma and prostate cancer.

 

Pegfilgrastim is a PEGylated form of the recombinant human granulocyte colony-stimulating factor (GCSF) analog filgrastim. It serves to stimulate the level of white blood cells (neutrophils).

Amgen manufactures pegfilgrastim under the brand name Neulasta Which was mainly worked on by Martine Allard, and Roche under the name Neulastim. In India it is also marketed by Abbott Healthcare under the brand name Imupeg. The drug is prepared by coupling a 20 kDa polyethylene glycol (PEG) molecule to the N-terminus of the filgrastim protein. Pegfilgrastim has a human half-life of 15 to 80 hours, much longer than the parent filgrastim (3–4 hours).

Pegfilgrastim treatment can be used to stimulate the bone marrow to produce more neutrophils to fight infection in patients undergoing chemotherapy.

 

AYURVEDA-Jyotishmati / Malkangani – Staff-tree (Celastrus paniculatus)



Jyotishmati / Malkangani -Staff-tree, (Celastrus paniculatus)

  • Excellent pain reliever

Relieves pain: Apply staff-tree oil on the affected area.

Celastrus paniculatus
Scientific classification
Kingdom: Plantae
(unranked): Angiosperms
(unranked): Eudicots
(unranked): Rosids
Order: Celastrales
Family: Celastraceae
Genus: Celastrus
Species: C. paniculatus
Binomial name
Celastrus paniculatus
Willd.
Synonyms
Celastrus dependens Wall.

Celastrus paniculatus seeds

Celastrus paniculatus is a woody liana commonly known as black oil plant, climbing staff tree, and intellect tree (Sanskrit: jyotishmati ज्योतीष्मती, Hindi: Mal-kangani माल-कांगनी, Chinese: deng you teng 灯油藤).[1][2][3] The plant grows throughout India at elevations up to 1800 m.[1][4] Oil from the seeds is used as a traditional medicine in Indian Unani and Ayurvedic medicine.[1][5]

C. paniculatus is a deciduous vine with stems up to 10 centimeters in diameter and 6 meters long with rough, pale brown exfoliating bark covered densely with small, elongated lenticles. The leaves are simple, broad, and oval, obovate or elliptic in shape, with toothed margins.[1][2] The Intellect tree, or Celastrus paniculatus, is a climbing shrub, also known as malkangani, found throughout India. The seeds contain fatty acids and alkaloids, and have sedative and antidepressant actions. Botanist M. Daniel states that the seeds are used to sharpen the memory, and Ayurvedic practitioners also use the seed oil as a brain tonic and as a treatment for memory loss. A study published in the August 2004 issue of the “Journal of Ethnopharmacology” found that intellect tree’s ability to improve memory loss may be due to its neuroprotective actions. A study of rats suggested the aqueous extract of Celastrus paniculatus seed has dose-dependent cholinergic activity, thereby improving memory performance.[6]

 

  1.  Premila, M. S. (2006). Ayurvedic Herbs: A Clinical Guide to the Healing Plants of Traditional Indian Medicine. New York: Haworth Press. ISBN 0-7890-1768-7.
  2. H. F. Macmillan (1989). Handbook of Tropical Plants. Columbia, Mo: South Asia Books. ISBN 81-7041-177-7.
  3.  Putz, Francis E.; Mooney, Harold A. (1991). The Biology of vines. Cambridge, UK: Cambridge University Press. ISBN 0-521-39250-0.
  4.  Zhixiang Zhang, Michele Funston: Celastrus, in Flora of China, Vol. 11
  5.  Chopra, R. N. Indigenous Drugs of india. Kolkata: Academic Publishers. ISBN 978-81-85086-80-4.
  6.  Bhanumathy M. Harish MS. Shivaprasad HN. Sushma G.”Nootropic activity of Celastrus paniculatus seed.Pharmaceutical Biology. 48(3):324-7, 2010 Mar.

Native to: India, China, Sri Lanka, and south-east Asia

 

Celastrus paniculatus is a shrub used in Ayurdevic medicine in India.  Various properties are attributed to the aerial parts of the plant, but we will deal here primarily with the seeds and the oil expressed from them. Celastrus paniculatus oil is cold-pressed raw herbal oil expressed from the Malkangni/Intellect Tree seeds of Celastrus panuculatis, a shrub native to India.   While Celastrus oil has been used in India for centuries it is only within the past few years that it has started to become known outside of Ayurvedic medicine, the traditional medicinal practice of India.

 

1.   The oil is used to increase memory and facilitate learning.

2.   It induces a feeling of well-being and has reported aphrodisiac effects.

The oil in its raw state has a shelf life of 2 years if kept in a cool and dark place such as a refrigerator. When put into softgels the shelf life can be expected to be much longer, on the order of four years if kept in a dark and refrigerated state.

Oil Chemical Composition:

The oil contains protein,   carbohydrates (less than 1 calorie per dose), fats (saturated fats: .022 of 1%, polyunsaturated fats: .035 of 1%, monounsaturated fats: .032 of 1%) Vitamin C, Sodium, Potassium, ash, Calcium, Iron, and Sesqiterpene polyesters.

Uses of Malkangni:

1.   Celastrus paniculata is a treasured medicinal herb that is revered for its effects on the brain and has been used for centuries in Ayurveda for sharpening the memory, increasing intellect, and improving concentration.

2.   The seed oil is used for massage with great benefit, especially in vata diseases like sciatica, lumbago, paralysis, arthritis and facial palsy.

3.   The seed oil is useful to hasten the healing in nonhealing wounds and ulcers.

4.   Essential for acne, boils, eczema and hair loss.

5.   Excellent pain reliever Relieves pain

The seed oil is extremely beneficial as a sirovirecana cleansing nasal therapy, wherein the drops instilled into nostrils, ward off mucous secretions in colds and cough.

Habitat:

It grows almost all over India, up to attitude of 1,800 meter Specially Punjab, Kashmir etc. hilly state. It is also found SriLanka, Malaya deep and Philippines.  Globally the species occurs in the tropical and subtropical regions of India, Myanmar (earlier Burma), China, Malaysia, SriLanka and Philippines and also in North America. Within India, it occurs in Andhra Pradesh, Karnataka, Goa, Maharashtra, Gujarat, Madhya Pradesh, Uttar Pradesh, Arunachal Pradesh, Punjab and Himachal Pradesh.

The leaf and seed of Jyotismati is used in the form of powder and oil to treat udara roga, wound, sidhma, drowsiness in fever and amenorrhoea and many Skin diseases.

Morphology Description:

Malkagni is a large, woody, climbing shrub. The leaves are ovate oblong-elliptic, the flowers are unisexual, small greenish white or yellowish green, the capsules are globose, yellow 1-6 seeded and transversely wrinkled, the seeds are ellipsoid or ovoid, yellowish or reddish-brown in color enclosed in scarlet aril, which stains yellowish orange.

Chemical Composition: 

The seeds yield brownish yellow oil 52.2% with an unpleasant taste. This oil is reported to contain acetic acids & benzoic acids in addition to the higher amount of the fatty acids.

Application:

The oil of Malkagini locally act as a good analgesic, anti-inflammatory it overcome pain and inflammation in case of paralysis, facial paralysis, joint pains, sciatica, lumber pain etc.

Ayurveda recognizes its seeds as an effective nervine tonic. Its use is recommended in chronic debilitating diseases of nervous system. The seeds possess emetic, diaphoretic, febrifugal and Nervine properties and are used for sharpening the memory & learning abilities.  

Effect on Doshas – Pacifies Vata & Kapha, Promotes Pitta.

Launch of semi-synthetic artemisinin a milestone for malaria, synthetic biology


Apr 11th, 2013

Launch of semi-synthetic artemisinin a milestone for malaria, synthetic biology

(Nanowerk News) Twelve years after a breakthrough discovery in his University of California, Berkeley, laboratory, professor of chemical engineering Jay Keasling is seeing his dream come true.
On April 11, the pharmaceutical company Sanofi will launch the large-scale production of a partially synthetic version of artemisinin, a chemical critical to making today’s front-line antimalaria drug, based on Keasling’s discovery.read more at nanowerk

http://www.nanowerk.com/news2/biotech/newsid=29955.php

The “semi-synthetic” artemisinin is chemically modified to an active drug, such as artesunate, and combined in ACT with another antimalarial drug to lessen the chance that the malaria parasite will develop resistance to artemisinin. Sanofi plans to produce 35 tons of artemisinin in 2013 and, on average, 50 to 60 tons a year by 2014, which will translate to between 80 and 150 million ACT treatments.

Sweet wormwood was used in ancient Chinese therapy to treat various illnesses, including fevers typical of malaria. In the 1970s, Chinese scientists rediscovered it and identified its active ingredient, artemisinin, and artemisinin is now extracted from sweet wormwood grown commercially in China, Southeast Asia and Africa. The quality, supply and cost have been unpredictable and inconsistent, however. Keasling’s goal was to create a synthetic version with a stable and ideally lower price that could be produced in sufficient quantity to treat the 300-500 million cases of malaria that arise each year.

Sanofi and OneWorld Health, the not-for-profit drug development affiliate of the Program for Appropriate Technology in Health (PATH), have launched a commercial-scale production line for semisynthetic artemisinin, a move they say is “a pivotal milestone in the fight against malaria”.

Global demand for artemisinin is the most effective malaria treatment available but the existing botanical supply – which is derived from the sweet wormwood plant – is inconsistent. Therefore, Sanofi says that having “multiple sources of high-quality artemisinin will strengthen the artemisinin supply chain, contribute to a more stable price and ultimately ensure greater availability of treatment”.

The company notes that the production line at its facility in Garessio, Italy, will be able to produce enough artemisinin, using technology developed by US firm Amyris, for around 80-150 million artemisinin-based combination therapies by 2014.

Otsuka’s New Drug Application for Tolvaptan, the Investigational Compound for Autosomal Dominant Polycystic Kidney Disease (ADPKD), Accepted for Review by the US Food and Drug Administration (FDA)


Otsuka Pharmaceutical Co., Ltd. announced today that the U.S. Food and Drug Administration (FDA) has accepted for priority review the company’s new drug application (NDA) for the potential use of tolvaptan for the treatment of autosomal dominant polycystic kidney disease (ADPKD). Phase III clinical trial results………..read more at financial post

http://www.financialpost.com/markets/news/Otsuka+Drug+Application+Tolvaptan+Investigational+Compound+Autosomal/8231579/story.html

Tolvaptan
and enantiomer
Systematic (IUPAC) name
N-(4-{[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide
Tolvaptan (INN), also known as OPC-41061, is a selective, competitive vasopressin receptor 2 antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan was approved by the U.S. Food and Drug Administration (FDA) on May 19, 2009, and is sold by Otsuka Pharmaceutical Co. under the trade name Samsca and in India is manufactured & sold by MSN laboratories Ltd. under the trade name Tolvat & Tolsama.

Merck seeks approval for pill form of antifungal,noxafil


Posaconazole is a triazole antifungal drug marketed in the United States, the European Union, and in other countries by Schering-Plough under the trade name Noxafil. In Canada, posaconazole is marketed by Schering-Plough under the trade name Posanol.

11 april2013

Merck & Co says that a New Drug Application for a tablet formulation of the company’s antifungal Noxafil has been accepted for review by the US Food and Drug Administration.

Merck currently markets Noxafil (posaconazole) in liquid form for invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being “severely immunocompromised”. This covers patients who have received haematopoietic stem cell transplants and have graft-versus-host disease, or patients with cancers of the blood who are experiencing prolonged low white blood cell counts as a result of chemotherapy.

Specifically, Merck is seeking FDA approval of Noxafil tablets for once-daily administration, following a twice-a-day loading dose on the first day of therapy. The pill has already been filed with the European Medicines Agency and the drug giant plans to seek regulatory approval for the tablet formulation in other countries around the world.

Robin Isaacs, head of infectious disease clinical research at Merck Research Laboratories, said the filing for a Noxafil pill “is an example of Merck’s ongoing commitment to developing new therapy options for patients in the hospital setting”. He added that “invasive fungal infections are a significant cause of illness and death among severely immunocompromised patients”.

ACADIA Pharmaceuticals announced , it no longer needs to conduct additional Phase III trials for its pimavanserin drug for the treatment of Parkinson’s disease psychosis


cas no 706779-91-1
706782-28-7 (tartrate)

11, april 2013

ACADIA Pharmaceuticals announced following its FDA meeting, it no longer needs to conduct additional Phase III trials for its pimavanserin drug for the treatment of Parkinson’s disease psychosis. The company plans to seek early approval for the drug.

ACADIA Pharmaceuticals Inc.  announced that the FDA has agreed that the data from the pivotal Phase III -020 study, together with supportive data from other studies with pimavanserin, are sufficient to support the filing of a New Drug Application, or NDA, for the treatment of Parkinson’s disease psychosis, or PDP. ACADIA will no longer conduct the Phase III -021 study that was planned as a confirmatory trial. ACADIA believes FDA decision will reduce substantially both the time and cost of the company’s PDP development program.

ACADIA is currently focused on completing the remaining elements of its pimavanserin PDP development program that are needed for submission of an NDA. ACADIA is currently targeting an NDA submission near the end of 2014.

Pimavanserin (ACP-103) is a drug developed by Acadia Pharmaceuticals which acts as an inverse agonist on the serotonin receptor subtype 5-HT2A, with 10x selectivity over 5-HT2C, and no significant affinity or activity at 5-HT2B or dopamine receptors.[1] As of September 3 2009, pimavanserin has not met expectations for Phase III clinical trials for the treatment of Parkinson’s disease psychosis,[2] and is in Phase II trials for adjunctive treatment of schizophrenia alongside an antipsychotic medication.[3] It is expected to improve the effectiveness and side effect profile of antipsychotics.[4][5][6]

  1.  Vanover KE, Weiner DM, Makhay M, Veinbergs I, Gardell LR, Lameh J, Del Tredici AL, Piu F, Schiffer HH, Ott TR, Burstein ES, Uldam AK, Thygesen MB, Schlienger N, Andersson CM, Son TY, Harvey SC, Powell SB, Geyer MA, Tolf BR, Brann MR, Davis RE (May 2006). “Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N’-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine2A receptor inverse agonist”. J Pharmacol Exp Ther 317 (2): 910–8. doi:10.1124/jpet.105.097006. PMID 16469866.
  2. ACADIA Pharmaceuticals. “Treating Parkinson’s Disease – Clinical Trial Pimavanserin – ACADIA”. Retrieved 2009-04-11.[dead link]
  3.  “ACADIA Announces Positive Results From ACP-103 Phase II Schizophrenia Co-Therapy Trial” (Press release). ACADIA Pharmaceuticals. 2007-03-19. Retrieved 2009-04-11.
  4.  Gardell LR, Vanover KE, Pounds L, Johnson RW, Barido R, Anderson GT, Veinbergs I, Dyssegaard A, Brunmark P, Tabatabaei A, Davis RE, Brann MR, Hacksell U, Bonhaus DW (August 2007). “ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental models”. J Pharmacol Exp Ther 322 (2): 862–70. doi:10.1124/jpet.107.121715. PMID 17519387.
  5.  Vanover KE, Betz AJ, Weber SM, Bibbiani F, Kielaite A, Weiner DM, Davis RE, Chase TN, Salamone JD (October 2008). “A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model”. Pharmacol Biochem Behav 90 (4): 540–4. doi:10.1016/j.pbb.2008.04.010. PMC 2806670. PMID 18534670.
  6.  Abbas A, Roth BL (December 2008). “Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders”. Expert Opin Pharmacother 9 (18): 3251–9. doi:10.1517/14656560802532707. PMID 19040345.