Happy 2021! Here’s the last installment of Small Molecules of the Month for 2020. It was so hard to narrow this down to one sheet of molecules since there were so many timely publications in December. One of my favorites this month is an oral(!) ultra-long acting insulin derivative from Novo which demonstrated human efficacy in Ph. II (and yes it’s still considered a small molecule). Another interesting one is the oral non-covalent HbS modulator from Pfizer, which binds in a 2-drugs-to-1-complex fashion similar to early analogs of the covalent drug voxelotor. There were also two TNFa asymmetric trimer stabilizers from AbbVie and BMS that you shouldn’t miss, and several candidates to note for important cancer targets (CDK9, ERK, PI3Ka, PARP, ER, and IDO1). Enjoy!

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Small Molecules of the Month - Dec. 2020

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Links to Articles:

  1. OI338 (Novo oral insulin analog)
  2. PF07059013 (Pfizer noncovalent oral hemoglobin (HbS) modulator)
  3. AZD0364 (AstraZeneca oral reversible ERK1/2 kinase inhibitor)
  4. PF-06843195 prodrug (Pfizer oral PI3ka-selective kinase inhibitor prodrug)
  5. TP0586352 (Taisho non-hydroxamate LpxC deacetylase inhibitor)
  6. AZD4573 (AstraZeneca selective CDK9 kinase inhibitor)
  7. “compound 42” (Bristol Myers Squibb (BMS) selective TNFα allosteric inhibitor)
  8. “compound 12” (AbbVie selective TNFα allosteric inhibitor)
  9. BMS-986202 (Bristol Myers Squibb (BMS) oral JH2-domain binding Tyk2 kinase inhibitor)
  10. pamiparib (Beigene oral, brain-penetrant PARP1/2 inhibitor/DNA trapping agent)
  11. linrodostat (Bristol Myers Squibb (BMS) oral selective heme-displacing IDO1 inhibitor)
  12. SAR439859 (Sanofi oral selective estrogen receptor (ER) degrader (SERD))
  13. ACT-1004-1239 (Idorsia/Actelion CXCR7 GPCR insurmountable antagonist)
  14. “compound 1” (Merck anion-dependent farnesyl transferase inhibitor)

Hope this was helpful, and have a great 2021. Again, if you have an extra moment, please take our 5 min survey. Explore drughunter.com for more.