First-time disclosure of Clinical Candidate live tweeting-UPDATED
Aug22

First-time disclosure of Clinical Candidate live tweeting-UPDATED

UPDATED: Sep. 7- You can now find structures for the drug candidates disclosed at the symposium in this pdf document. UPDATED: Aug. 24- Structure of Pfizer drug is incorrect. Will re-post shortly. 2:01:27 PM: Hello, this is Leigh Krietsch Boerner live tweeting from the First-time Disclosure of Clinical Candidate session at #acs_bsoton #acsmedi2:02:31 PM: First up is David Millan from Pfizer #acs_boston #acsmedi2:04:11 PM: The name of the drug is PF-037154552:04:32 PM: The name of the drug is PF-03715455 #acs_boston #acsmedi2:05:51 PM: It's used to treat chronic obstructive pulmonary disease (COPD), which affects 30 million people worldwide #acs_boston #acsmedi2:07:41 PM: It's a p38 inhibitor, which is expressed and activated in the lungs of COPD patients #acs_boston #acsmedi2:33:35 PM: Structure of Pf-03715455 #acs_boston #acsmedi 2:34:39 PM: Next up is Michael Sofia from Pharmasset, Inc. #acs_boston #acsmedi2:35:29 PM: The name of the drugs are PSI-352938 and PSI-353661 #acs_boston #acsmedi2:36:14 PM: It's to treat Hepatitis C, or HCV, which affects 180 million people worldwide. #acs_boston #acsmedi2:48:51 PM: The target is NS5B-RdRP, which is part of the RNA genome of the HCV virus #acs_boston #acsmedi3:07:11 PM: Both drugs are 2'-alpha-F, 2'-beta-C-methyl nucleoside class #acs_bsoton, #acsmedi3:09:44 PM: PSI-352938 is in phase 1b clinical trials, PSI-353661 entering phase 1 #acs_boston #acsmedi3:10:18 PM: Next up is Dr. Orn Almarsson #acs_boston, #acsmedi3:11:54 PM: He is from Alkermes, which is a biotechnology company #acs_boston #acsmedi3:13:07 PM: They are working towards treatments for reward/impulse control disorders ie substance abuse, binge eating, etc #acs_boston #acsmedi3:14:35 PM: Target is opiod modulation #acs_boston #acsmedi3:16:05 PM: Will discuss ALKS 33 #acs_boston #scsmedi3:27:26 PM: Attenuates dopamine release in the NAc shell stimulated by ethanol, AMPH and cocaine #acs_boston #acsmedi3:27:55 PM: Range from phase 1 studies to phase 2/3 #acs_boston #acsmedi3:31:52 PM: Phase 2/3 is in alcohol dependance adaptive trial. #acs_boston #acsmedi3:32:55 PM: Partial kappa-opiod agonist, partial delta-opiod agonist/antagonist, potent mu-opiod antagonist #acs_boston #acsmedi3:33:53 PM: Next talk is Vincent Mascitti, discovery of nes class of SGLT2 inhibitors, from Pfizer #acs_boston #acsmedi3:34:34 PM: Phase 2, bridged ketal series, dioxa-bicyclo[3.2.1]octane motif #acs_boston #acsmedi3:35:19 PM: SGLT2 is sodium glucose co-transporter 2 to treat type 2 diabetes #acs_boston #acsmedi3:37:09 PM: for review of natural product synthesis, see Washburn, W.N. J Med Chem 2009 52, 1785 #acs_boston #acsmedi3:50:59 PM: Another paper on these molecules is V. Mascitti & C. Prville Org Lett, 2010, 12 (13), pp 2940–2943 http://bit.ly/bvdHNS #acs_boston #acsmedi3:59:59 PM: Last talk of the session is Paul Watson from Inspire Pharmaceuticals, Inc. #acs_boston #acsmedi4:01:01 PM: The drug is INS115644 (latrunculin B) #acs_boston #acsmedi4:01:36 PM: It's to treat glaucoma, which is an optic neuropathy that can cause vision loss. #acs_boston #acsmedi4:07:54 PM: Target inhibitors of actomyosin contractilily and inhibitors of...

Read More
Liveblogging Open Science Summit-Open Source Drug Discovery
Jul31

Liveblogging Open Science Summit-Open Source Drug Discovery

12:46:59 PM: Hi from Berkeley, California- I'm at the Open Science Summit http://bit.ly/b4NRq1. Tweets on open innovation and drug discovery to follow!12:51:12 PM: Aiden Hollis of Yale's Health Impact Fund is first http://bit.ly/Msd2N.12:53:00 PM: Fund aims to reward pharma co's based on drugs' health impact, if companies agree to sell at cost. Financing would come from government.12:58:32 PM: Health Impact Fund is planning a pilot project- but companies, countries, and drugs to be involved weren't specified. #oss201012:59:54 PM: RT @uaem: Jamie Love, from here: http://bit.ly/cKAEcn talking re: prizes to de-link cost of R&D from the cost of the final product #oss20101:05:11 PM: Love is again talking about rewarding a drug's 'health impact'. This is nebulous to me. How do you measure this impact a priori? #oss20101:15:04 PM: RT @OrthoNormalRuss: @carmendrahl when someone makes such vague assertions, they call them "details to be hashed out later" by some agency1:16:56 PM: Love's talk was rich in econ-speak but vague on details- more may be found here: http://bit.ly/9UGbPL in a comment sent to WHO #oss20101:27:35 PM: Columbia U GS @OrthoNormalRuss is sad this session didn't really deliver novel alternatives for R&D funding- same old gov't $$ arguments.1:39:15 PM: If you'd like to follow the Summit live you can at http://bit.ly/d2t4JC #oss2010 (Thx to Lisa Green, Creative Commons @boudicca for link)1:48:19 PM: Next session is called 'Cure Entrepreneurs': first speaker is Scott Johnson, prez of Myelin Repair Foundation. http://bit.ly/7VK9K1:52:03 PM: RT @mrgunn: Patient activism session up now. These folks tend to be passionate, so tune in now. #oss20101:54:46 PM: Johnson is describing the gap that exists between basic academic research, and research in pharma that leads to medications.1:58:33 PM: Johnson sees nonprofits like Myelin Found. as a shepherd-herd molecules through R&D through the approval process.2:04:34 PM: Myelin Foundation currently funding ~45 scientists. Universities own any patents, foundation has exclusive development rights.2:06:22 PM: Johnson says it's hard to get federal funding for developing tools and models for myelin repair research. Really? #oss20102:08:54 PM: Johnson-1st patent from these efforts awarded in 2008. A partnership with a pharma company (unnamed) has also been initiated.2:11:40 PM: Myelin repair drugs would treat multiple sclerosis: read @lisamjarvis #CENews story on race to new MS drugs http://bit.ly/9Iaz7N #oss20102:14:18 PM: Next: Craig Benson, founder of foundation to accelerate treatments for Batten Disease, rare neurodegenerative disease http://bit.ly/9eM05S2:19:38 PM: Among Beyond Batten's goals: developing accessible screens to test for carriers of orphan diseases like Batten2:21:09 PM: Benson has a daughter with Batten Disease. Johnson has multiple sclerosis.2:28:01 PM: Benson-Foundation dev'd a universal carrier screening test for 450 orphan diseases for under $500. Product launch planned for 2011 #oss20102:34:12 PM: More details on Benson...

Read More
Liveblogging 1st Disclosures of Drug Candidates
Mar21

Liveblogging 1st Disclosures of Drug Candidates

UPDATE April 2: If you read this coverage please tell us what you thought about it here or in the comments. 1:26:15 PM: I'm @ Moscone Ctr in San Fran. T minus half hour to unveiling of new drug candidate structures. #acsmedi #acs_sf1:37:35 PM: A hearty welcome to any readers of Totally Synthetic @Totsyn #acsmedi2:01:50 PM: 1st: Albert J. Robichaud-of Lundbeck-on Pfizer's $PFE SAM-531, 5-HT6 antagonist for schizophrenia, Alzheimer's #acsmedi #acs_sf2:02:53 PM: Alzheimer's therapies today- palliative. Modulate eiether acetylcholine, glutamate #acsmedi #acs_sf2:04:58 PM: ~45 million ppl with ALzheimer's worldwide- patients have probs w learning,memory, reasoning #acsmedi #acs_sf2:06:33 PM: 5HT6- 1 of 14 serotonin receptors- a G-protein coupled receptor #acsmedi #acs_sf2:07:00 PM: block 5HT6- boosts levels of glutamate, acetylcholine neurotransmission in brain areas assoc w/learning, memory #acsmedi #acs_sf2:09:37 PM: focus has been indole, azaindoles #acsmedi #acs_sf2:09:47 PM: http://twitpic.com/1a3b3v - Lead2:12:17 PM: SAR: aryl sulfonyl groups req'd for activity. Most substitution not good on indole NH. #acswmedi #acs_sf2:15:13 PM: http://twitpic.com/1a3c9x - 5312:16:59 PM: SAM-531 enhances memory retention in rodents in a test called novel object recognition #acsmedi #acs_sf2:18:46 PM: SAM-531 potent selective 5HT6 antagonist. In phase II clinical development in patients with Alzheimer's #acsmedi #acs_sf2:21:00 PM: Q&A: what is brain to plasma ratio? speaker says less than 25%. But high enough for efficacy2:22:20 PM: pKa of the amine in metabolites? HERG inhibition? pKa wasn't known. No issues with HERG.2:22:37 PM: Next: Thomas Simpson of AstraZeneca $AZN on AZD2624, NK3 receptor antagonist to test NK3 hypothesis in schizophrenia #acsmedi #acs_sf2:22:46 PM: Astrazeneca on Twitter @AstraZenecaUS2:23:22 PM: Schizophrenia: 2.2 million people in US have it #acsmedi #acs_sf2:23:43 PM: Schiz. drugs (many are dopamine receptor antagonists) aren't equally effective @ treating all symptoms #acsmedi #acs_sf2:24:49 PM: NK3 blockers adjust dopamine levels by indirect mechanism- new opportunities #acsmedi #acs_sf2:25:41 PM: Phase II studies on osanetant and talnetant- NK3r blockers- precedents in clinic #acsmedi #acs_sf2:27:24 PM: both osenetant and talnetant are no longer in development- but support idea of NK3 #acsmedi #acs_sf2:28:50 PM: Talnetant is a more druglike structure than osanetant #acsmedi #acs_sf2:29:55 PM: Improve solubility and plasma protein binding of talnetant. A poster later today will outline early chem strategy. #acsmedi #acs_sf2:32:32 PM: http://twitpic.com/1a3g8v - T2:33:19 PM: http://twitpic.com/1a3gfd - O2:33:42 PM: Patnent #s WO2006130080, 137789, WO200703528 #acsmedi, #acs_sf2:35:44 PM: Sulfonate ester - this path leads to clinical candidate #acsmedi #acs_sf stability was an issue-hydrolysis2:37:31 PM: http://twitpic.com/1a3hcu - Sulf es2:38:49 PM: Alkylsulfonylamino groups- dramatic improvement in stability #acsmedi #acs_sf2:39:52 PM: 2624- gerbil brain/plasma: 0.21 #acsmedi #acs_sf2:40:12 PM: http://twitpic.com/1a3hyj - 26242:43:40 PM: Comparing a sulfoxide, AZD9122: half life (h): 2.8 rat, 6.7 dog. 2624 is better: 3.2 rat, 9.something in dog #acsmedi #acs_sf2:45:22 PM: in monkeys: AZD2624...

Read More