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. Unfo...

This month features some remarkable molecules including an allosteric pan-mutant isoform-selective PI3Kα inhibitor, a potentially best-in-class CNS-penetrant PARP1 inhibitor and trapper, and a photosw...

There are three notable highlights from AbbVie this month with published details on their first-in-class PTPN2/N1 inhibitor ABBV-CLS-484, currently in Phase I trials, and their recently acquired PINK1...

This month features many molecules in Phase III clinical trials including Calcilytix’s CaSR antagonist for hypocalcemia and DalCor Pharma’s repurposed CETP inhibitor to treat cardiovascular disease. W...

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...

This month features big announcements from Biogen on their acquisition of Reata and their Nrf2 activator for Friedreich’s ataxia and from BridgeBio on their TTR stabilizer with positive Ph. III data f...

With the popular success of diabetes and weight-loss peptide drugs from Novo (e.g. semaglutide/Ozempic), this month features a pair of ultra-hot non-peptide oral GLP-1R modulators in clinical developm...

An oral, potentially CNS-penetrant BTK inhibitor for multiple sclerosis, a reversible pan-KRAS inhibitor, and a squaramide-containing clinical candidate are just some of the examples for this month's...

An oral macrocyclic peptide PCSK9 inhibitor entering Ph. III for hypercholesterolemia later this year, a Ph. I/Ib KRASG12C(ON) tri-complex inhibitor for the treatment of advanced solid tumors, an oral...

A Ph. IIb TYK2 inhibitor from Nimbus (just bought by Takeda) that may be more efficacious than deucravacitinib, the first and only approved CGRP receptor antagonist nasal spray for the treatment of ac...

A Merck HIV inhibitor with targeted cell-killing activity as a possible approach to finally eradicate HIV, a KIT-selective inhibitor with best-in-class potential for the treatment of GIST, a first-in-...

The first, approved non-covalent BTKi, a next-generation oral SERD, a bioactive metabolite of a GHSR1a inverse agonist with the same therapeutic effect but different MOA to its parent are just some of...

We asked the drug discovery community to nominate molecules for our annual Molecule of the Year spot based on what you found most technically impressive and impactful. Here is the final list of the to...