Molecules of the Month

December 2023

December 2023 was a big month for estrogen receptor (ER) degraders featuring stories from Phase III candidates vepdegestrant, camizestrant, and OP-1250 (not included here) to treat breast cancer. Unfortunately, Phase II trials of Boehringer Ingelheim’s selective ENaC inhibitor, BI 1265162, to treat CF and Phase III trials of Serono’s much anticipated BTK inhibitor, evobrutinib, to treat MS were both terminated. Additionally, preclinical candidates from Genentech and Roche, promising Phase II candidates to treat myelodysplastic syndrome and atrial fibrillation, and a Phase III candidate to treat CLL/SLL are featured this month.

We’ll have more detailed case studies on these molecules coming soon, but in the meantime, you can check out some recent articles about the following here:

  1. AG-946 - An oral allosteric activator of wild-type and mutant PKR currently in Phase II for myelodysplastic syndromes, developed by Agios in Cambridge, MA.

  2. GNE684 - A preclinical oral RIP1 inhibitor was published. Genentech has also reported GDC-8264, an oral RIP1 inhibitor, in Phase Ib for acute graft-versus-host disease (aGVHD).

  3. lisaftoclax - An oral selective BCL-2 inhibitor currently in Phase III for chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), developed by Ascentage in Suzhou, CN and Rockville, MD.

  4. BI 1265162 - An inhaled selective ENaC inhibitor developed by Boehringer Ingelheim in Biberach, DE was terminated in Phase II for cystic fibrosis.

  5. evobrutinib - An oral selective irreversible BTK inhibitor developed by EMD Serono/Merck KaA was terminated in Phase III trials for multiple sclerosis.

  6. compound 18 - A preclinical oral brain-penetrant selective irreversible AEP inhibitor was published by Roche in Basel, CH. 

  7. vepdegestrant - An oral CRBN-based heterobifunctional estrogen receptor (ER) degrader developed by Arvinas currently in Phase III for advanced breast cancer.

  8. TM38837 – An oral peripherally restricted CB1 antagonist that was identified by reducing the lipophilicity of CNS-penetrant rimonabant.

  9. AP30663 - A negative allosteric modulator of KCa2 channels that has completed Phase II for atrial fibrillation, developed by Acension in Copehagen, DN.

  10. camizestrant - An oral selective estrogen receptor (ER) degrader developed by AstraZeneca that is currently in Phase III for breast cancer.

Stay tuned to read the Drug Hunter case studies on these molecules.

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