Molecules of the Month

August 2023

This month features many of the big reveals from the ACS fall 2023 first disclosures including Nurix’s BTK degrader and RAPT’s CCR4 autoimmune therapy. Several of the molecules making the August list are in Ph. III clinical trials such as Vertex’s sodium channel inhibitor for acute pain and Denali Therapeutics’ CNS-penetrant eIF2B activator for ALS. 

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. VX-548 - oral NaV1.8 selective inhibitor developed by Vertex Pharmaceuticals for acute pain in Phase III clinical trials.

  2. STX-478 - mutant-selective, allosteric PI3Ka inhibitor developed by Scorpion Therapeutics for breast cancer and other solid tumors in Phase I/II clinical trials.

  3. JNT-517 - oral allosteric SLCA6A19 inhibitor developed by Jnana Therapeutics for PKU in Phase Ib clinical trials.

  4. NX-5948 - oral BTK degrader developed by Nurix Therapeutics for B-cell malignancies in Phase I clinical trials.

  5. RPT193 - oral selective CCR4 antagonist developed by RAPT Therapeutics for atopic dermatitis and T2-high asthma in Phase II clinical trials.

  6. PF-9363 - oral selective KAT6A/B inhibitor developed by Pfizer and Cancer Therapeutics for ER+ HER2 breast cancer in Phase I clinical trials.

  7. muvalaplin - oral Lp[a] disruptor developed by Eli Lilly for ASCVD in Phase II clinical trials.

  8. DNL343 - oral CNS-penetrant eIF2B activator developed by Denali Therapeutics for ALS in Phase II/III clinical trials.

  9. divarasib - oral selective covalent KRAS(G12C) inhibitor developed by Genentech for NSCLC in Phase III clinical trials.

  10. milademetan - oral MDM2 inhibitor discovered by Daiichi Sankyo and developed by Rain Oncology for metastatic solid tumors in Phase II clinical trials.

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