Arcus CD73 inhibitor (Arcus non-nucleoside CD73 inhibitor)

MK-6884 (Merck M4 positive allosteric modulator PET tracer) 2022 Update: Human Ph. I data disclosed in https://doi.org/10.1126/scitranslmed.abg3684

Sulfopin (Weizmann/Harvard selective covalent Pin1 inhibitor)

M3814 (Merck KGaA oral DNA-PK selective kinase inhibitor)

Remibrutinib (Novartis oral BTK-selective covalent kinase inhibitor clinical candidate)

LMB763 (nidufexor) (Novartis (GNF) oral in vivo selective FXR partial agonist)

ABBV-744 (AbbVie oral in vivo BD2 domain selective BET inhibitor)

AG-881 (vorasidenib) (Agios oral brain penetrant allosteric mutant IDH1/2 dual inhibitor clinical candidate)

FT-2102 (olutsidenib) (FORMA oral allosteric mutant-selective IDH1 inhibitor clinical candidate)

GS-9876 (lanraplenib) (Gilead Sciences oral SYK selective kinase inhibitor clinical candidate)

KRAS(G12C) inhibitor from AZ (AstraZeneca oral in vivo mutant KRAS(G12C) allosteric covalent inhibitor)

RORγt inhibitor from Merck (Merck ROR-gamma-t oral in vivo allosteric inhibitor)

(Novartis (GNF) oral in vivo RET kinase inhibitor)

BMS-986260 (Bristol Myers Squibb (BMS) oral in vivo selective TGF-beta-R1 kinase inhibitor)

GNF2133 (Novartis (GNF) oral in vivo GSK3-beta-sparing DYRK1A kinase inhibitor)

The first disclosures of new drug candidates are always the highlight of medicinal chemistry conferences. Six novel drug candidates were recently disclosed by European companies at the European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (EFMC-ISMC) Conference in [...]

Recently, our team at Drug Hunter compiled the lead programs and mechanisms of small molecule and large molecule biotechs that IPO’d in 2020. We asked featured reviewers from our community what stood out to them about the science of this group of companies, and here are some highlights that emerged from the discussion. Any thoughts and [...]

The September edition of Small Molecules of the Month, features a number of fascinating molecules and mechanisms, including a beta-lactamase inhibitor optimized to have single agent antibiotic activity, a biased agonist of S1P1 that minimizes receptor internalization in favor of GCPR agonism, an oral AR degrader similar to ARV-110 and a molecule that unfortunately demonstrates QTc prolongation in vivo without a significant in vitro signal. Special thanks to reviewer Mike Koehler for commentary on the cover molecule, ETX0462, this month....