RG6537 / Roche, Shanghai Jeyou Pharmaceutical - LARVOL DELTA

GDC-2992: A heterobifunctional Androgen Receptor (AR) antagonist and degrader for the treatment of AR wild-type and mutant prostate cancer (AACR 2025) - P1 | "Co-treatment of GDC-2992 with the CRBN ligand pomalidomide prevents AR degradation mediated by GDC-2992 in vitro, supporting the role of CRBN in GDC-2992-mediated AR degradation. An ongoing Phase I dose-escalation and expansion study will assess the safety, tolerability, pharmacokinetics, and preliminary anti-tumor activity of GDC-2992 in patients with advanced or metastatic prostate cancer who have previously received AR-targeted therapy [NCT05800665]. By providing more complete and sustained AR inhibition, GDC-2992 has the potential to reduce the occurrence of treatment-resistance and disease relapse in prostate cancer."

Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • CRBN

A Study Evaluating the Safety, Pharmacokinetics, and Activity of RO7656594 In Participants With Advanced or Metastatic Prostate Cancer (clinicaltrials.gov) - P1 | N=210 | Recruiting | Sponsor: Genentech, Inc. | Trial completion date: Jul 2026 ➔ Jun 2027 | Trial primary completion date: Jul 2026 ➔ Jun 2027

Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

A Study Evaluating the Safety, Pharmacokinetics, and Activity of RO7656594 In Participants With Advanced or Metastatic Prostate Cancer (clinicaltrials.gov) - P1 | N=210 | Recruiting | Sponsor: Genentech, Inc. | N=160 ➔ 210

Enrollment change • Genito-urinary Cancer • Oncology • Prostate Adenocarcinoma • Prostate Cancer • Solid Tumor

Stereoselective Synthesis of trans-3-Amino-2,2,4,4-tetramethylcyclobutanol. (PubMed, Org Lett) - "Herein, we describe its development from inexpensive 2,2,4,4-tetramethylcyclobutane-1,3-dione, evolving from a poorly selective and stoichiometric oxime reduction to an efficient sequence of chemo- and biocatalytic reactions. The utility of this process, which also resulted in a 10-fold improvement in process mass intensity (PMI), was demonstrated on scale en route to a fragment of the investigational androgen receptor degrader GDC-2992."

Journal • AR

Comparing and Contrasting BMS-986365 and JMKX002992 and other AR degraders for prostate cancer (DAVAGU 2024) - No abstract available.

Clinical

Jemincare Announces Exclusive License Agreement with Genentech (PRNewswire) - "Jemincare...announced today that it and its subsidiary company, Shanghai Jemincare Pharmaceutical Co., Ltd., have signed a worldwide exclusive license agreement with Roche...and Genentech, a member of the Roche Group , for the development and commercialization of its androgen receptor degrader, JMKX002992....Under the terms of the agreement, Genentech will receive an exclusive license to develop and commercialize the downgrader worldwide, and will be fully responsible for development and commercialization costs. In exchange, Genentech will pay Jemincare an initial payment of US$60 million. Jemincare is also entitled to receive up to $590 million in additional payments if certain sales, regulatory and development milestones are met. Jemincare is also entitled to receive tiered royalties on net sales."

Licensing / partnership • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A Study Evaluating the Safety, Pharmacokinetics, and Activity of RO7656594 In Participants With Advanced or Metastatic Prostate Cancer (clinicaltrials.gov) - P1 | N=160 | Recruiting | Sponsor: Genentech, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Metastases • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A Study Evaluating the Safety, Pharmacokinetics, and Activity of RO7656594 In Participants With Advanced or Metastatic Prostate Cancer (clinicaltrials.gov) - P1 | N=160 | Not yet recruiting | Sponsor: Genentech, Inc.

Metastases • New P1 trial • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor