molecules of the month

October 2021

The October edition of Small Molecules of the Month includes several potential best-in-class clinical candidates including but not limited to a second-gen LPA1 antagonist from BMS, two muscle modulators from Cytokinetics, and a Janssen pan-genotype, pan-serotype Dengue virus inhibitor. There are several interesting modalities including an oral macrocyclic peptide from Merck, a tumor-specific prodrug from BMS, and a CRBN-based degrader that no-longer needs two imide motifs from St. Jude. As always, there’s plenty of interesting chemical groups – a hydrazine, furenone, pyrrole, decalin, strained macrocycle, quaternary ammonium, … enjoy!

Full summaries, a PDF download, and links to articles are below. Reviewer Joachim Rudolph also points us in the direction of MRTX1133, a potent KRAS G12D inhibitor which was recently disclosed at an AACR-NCI-EORTC virtual conference, but has not been published at the time of this article's publication.

A slide deck with more details about each molecule is available.

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past molecules of the month

Check out previous selections below.

molecules of the year nominees

Previous selections for Drug Hunter’s Molecule of the Year below.

hall of fame
molecules of the year

Previous selections for Drug Hunter’s Molecule of the Year below.




  • Johnson & Johnson
  • Roche
  • Pfizer
  • Novartis
  • Bayer
  • Merck
  • Sanofi
  • GlaxoSmithKline
  • AbbVie
  • Eli Lilly
  • Boehringer Ingelheim
  • Amgen
  • Bristol-Myers Squibb
  • Gilead
  • AstraZeneca
  • Teva
  • Novo Nordisk
  • Merck KGaA
  • Takeda
  • Celgene (BMS)
  • Biogen
  • Astellas
  • Daiichi Sankyo
  • Regeneron
  • UCB
  • Eisai
  • Servier
  • Kyowa Kirin
  • Shionogi
  • Vertex
  • Lundbeck
  • Taisho
  • Ono
  • Seagen
  • Incyte
  • LEO Pharma
  • Janssen
  • Galapagos
  • Idorsia
  • Astex
  • Arvinas
  • Kymera
  • Relay
  • Schrodinger
  • Mirati
  • Revolution
  • Nimbus
  • Plexxikon
  • Forma
  • Arcus
  • RA Capital
  • ARCH Venture Partners
  • MPM Capital
  • Orbimed
  • The Column Group
  • 5AM Ventures
  • Versant Ventures
  • Deerfield
  • Goldman Sachs
  • Citi
  • Piper Sandler
  • Softbank
  • …and hundreds of others