CC-90011 (Celgene/Bristol Myers Squibb (BMS)) selective, reversible LSD1 inhibitor clinical candidate)

CG428 (Cullgen CRBN-based TRK kinase fusion protein degrader)

“compound 34” (Lupid oral in vivo PARP1-selective polymerase inhibitor)

LEO 39652 (LEO Pharma “dual-soft” topical PDE4 inhibitor soft drug clinical candidate)

AG-636 (Agios Pharmaceuticals dihydroorotate dehydrogenase (DHODH) inhibitor clinical candidate)

“EST73502” (ESTEVE oral dual mu-opioid receptor agonist, sigma-1 receptor antagonist clinical candidate)

“compound 46” (Janssen oral selective brain-penetrant PDE2A phosphodiesterase inhibitor)

“compound 25” (Genentech IRE1 alpha kinase-binding endonuclease inhibitor)

“lipid 10a” (Arcturus tunable lipid for RNA drug delivery)

BAY-6672 (Bayer oral in vivo prostaglandin F receptor GCPR antagonist)

“compound 27” (Sanofi oral in vivo pan-PIM kinase inhibitor)

October’s molecule, the Bayer hGnRH-R antagonist BAY 1214784 , is intended as an oral, once-daily treatment for uterine fibroids, a highly common problem in adult women that can lead to infertility. Existing treatments include hGnRH-R blockers which have undesirable side effects such as induction of menopausal symptoms due to their influence [...]

BAY 1217224 (Bayer oral non-prodrug thrombin (Factor IIa) inhibitor)

FGF401 (roblitinib) is a highly selective, reversible-covalent inhibitor of the kinase FGFR4, a receptor that can drive progression of certain cancers. The Novartis team found that the FGFR4 protein has a high re-synthesis rate and therefore would require significant drug exposure to have a meaningful effect, so they deprioritized [...]

TNO155 is an allosteric inhibitor of the SHP2 phosphatase, which has been a hot target in oncology recently due to its promotion of mutant KRAS activity as well as its potential role in cancer immune evasion. Phosphatases have been notoriously difficult to drug however, with reported phosphatase active site inhibitors typically having low [...]

BMS-986143 is a potent, reversible inhibitor of the Bruton’s tyrosine kinase (BTK), which has been successfully targeted by a number of irreversible drugs for oncology. The safety bar is much higher for inflammatory conditions, however, which led the BMS team to pursue reversible inhibitors. The two defined axial stereocenters of compounds [...]

AZD9833 is a potent, orally available selective estrogen receptor degrader (SERD) and antagonist in development for breast cancer. The only approved SERD is the widely used fulvestrant, which is given by monthly intramuscular injection and may have submaximal antitumor activity. A safe, oral alternative has been highly sought after and the [...]

AL-611 is a prodrug to a nucleoside inhibitor of HCV NS5B polymerase. While there have been very successful nucleoside drugs (e.g. sofosbuvir), several nucleoside inhibitors of HCV previously failed in the clinic due to severe toxicities, in some cases due to incorporation of the nucleosides into host RNA. The Janssen Biopharma (formerly [...]