Hunter Batchelder

The Drug Hunter team is piloting a new series highlighting notable disclosures in the patent literature to provide our readers a timely and scientifically flavorful synopsis of therapeutic targets being actively pursued, emerging industry breakthroughs, and fascinating chemical matter. Here we highlight 12 patents published in December 2023 that piqued our interest, and compiled a searchable table comprising key information from more than 180 additional patents of potential interest to drug hunters. If you have any suggestions on how to make this more useful, please let us know!

The team reviews hundreds of compounds from thousands of papers, press releases, and other sources each month to select candidates for Molecules of the Month. Here we have compiled a table of >60 additional molecules that were of interest in December 2023 along with highlights from some of the team’s favorites in the article.

RAPT Therapeutics, formerly known as FLX Bio, was spun out of Flexus Biosciences after its billion-dollar acquisition by BMS for Flexus’s immuno-oncology IDO1 program. While the IDO1 molecule unfortunately did not show efficacy in Ph. III trials in combination with BMS’s PD-1 inhibitor nivolumab, RAPT Therapeutics appears to be having better luck with its potentially first-in-class CCR4 inhibitors FLX475 (for immune-oncology) and RPT193 (for atopic dermatitis). Oral FLX475 (100 mg QD, human T1/2 = 72 h) appears to shrink EBV+ tumors both as a monotherapy and in combination

The arachidonic acid (AA) metabolite, 20-hydroxy-5,8,11,14-eicosatetranoic acid (20-HETE), has been extensively studied as a modulator of kidney function and a mediator of kidney diseases over decades. The receptor for 20-HETE, the G-coupled protein receptor GPR75, was only recently identified (2017), and GPR75/20-HETE pathway modulators are of industry interest in many disease areas including obesity (e.g. 2020 Regeneron patent filing) and kidney diseases (e.g. 2018 Taisho patent filing).

PF-07054894 is a potential first-in-class, oral Ph. I clinical candidate targeting the chemokine receptor CCR6 for ulcerative colitis (NCT05549323). Several companies have pursued antibodies and small molecules targeting CCR6 or its endogenous ligand, CCL20 (e.g. GSK3050002) for immunological conditions including other preclinical squaramides (e.g. Galderma, Allergan, ChemoCentryx) and other series (e.g. Takeda), but PF-07054894 appears to be the first selective CCR6 antagonist to enter clinical development.