molecules of the month


IV AKR1C3-activated cytotoxin prodrug

Ph. I/II in advanced solid tumors

prodrug of DNA cross-linking agent

Br. J. Cancer, May 12, 2023

OBI Pharma, TW; Threshold Pharma, CA

OBI-3424 , AKR1C3-activated prodrug, IV AKR1C3-activated cytotoxin prodrug, Ph. I/II in advanced solid tumors, prodrug of DNA cross-linking agent, Br. J. Cancer, May 12, 2023 OBI PHARMA, TW; THRESHOLD PHARMA, CA
5 mins read

A diaziridine-based tumor-activated prodrug for AKR1C3-expressing cancers from a defunct Bay Area biotech. OBI-3424 (formerly TH-3424) is a tumor-activated prodrug in Ph. II that releases DNA-crosslinking diaziridine phosphamide (remniscent of thioTEPA) upon activation by the NAD(P)H-dependent aldoketoreductase, AKR1C3, which is differentially expressed in many cancers. The molecule was originated at Threshold Pharma in South San Francisco, a company led by former UCSF Vice Chancellor Barry Selick that focused initially on hypoxia-activated prodrugs like EGFRi-releasing tarloxitinib bromide (TH-4000) and nitroimidazole mustard evofosfamide (partnered with Merck KGaA but returned after Ph. III failure). The developers believe that OBI-3424 could distinguish from traditional phosphamide mustard agents, which alkylate and cross-link DNA at guanine at N7, by being more specific for tumors that express…

request a trial

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.

already a member? log in: