Novartis' AR-Targeting PROTAC JSB462 (ARV-766) Receives First Clinical Approval in China for Prostate Cancer

On August 11, the CDE official website showed,NovartisJSB462 Tablets Approved for Clinical Use, Indications are：1）Lutetium (177Lu) vipivotide tetraxetan for treatmentProstate-Specific Membrane Antigen with Prior Exposure to At Least One Androgen Receptor Pathway Inhibitor（PSMA）Positive Metastatic Castration-Resistant Prostate Cancer（mCRPC）Adult patients; 2)Combination of Abiraterone for the Treatment of High-Volume Metastatic Hormone-Sensitive Prostate Cancer（mHSPC）Adult Patients。

JSB462 is a targeted androgen receptor（AR）Protein Degradation Targeting Chimera（PROTAC）. Currently, it is in Phase II clinical trials overseas.

Source: CDE Official Website

JSB462（ARV766）It is a product developed by Arvinas.Novel, Potent Oral AR PROTAC, which can target wild-type AR and clinically relevant ARLigand Binding Domain（LBD）Mutants, including L702H, H875Y, T878A.

In April 2024, Novartis$1.16 billionThe price fromArvinas has introducedGlobal development and commercialization rights for JSB462, as well as all rights to the preclinical project AR-V7.

Arvinas at 2024 ASCO Conference AnnouncedLatest I/II Phase Clinical Data of JSB462 for the Treatment of mCRPC(Registration Number:NCT05067140）As of April 15, 2024, the study had enrolled a total of 123 subjects, including 53 subjects carrying AR LBD mutations.

The results showed that, in 47 patients with prostate-specific antigen（PSA）LevelEvaluatableofIn AR LBD mutation subjects,PSA50 response rate was 43%In terms of safety, it was well-tolerated, with no DLTs occurring.

Insight database shows that currently there are 44 globally.PaymentAR PROTAC Under Research, where BMS developedGridegalutamide is the fastest-progressing globally, currently in Phase III clinical trials.

In ChinaAR PROTAC under researchThere are 22 products., seven of which have entered the clinical stage, includingHRS-5041 (Hengrui),GT20029 (Kintor Pharmaceuticals),QLH12016 (Qilu Pharmaceutical),HP518 (HaiChuang Pharmaceuticals), SHR3591 (HengRui),HSK38008(Haisco), and RG6537 (Jimin可信).

Source: Insight Database

It is worth mentioning that,Global Development and Commercialization Rights of RG6537 SuccessfullyIn August 2022, it was exclusively licensed to Genentech, a subsidiary of Roche, with an upfront payment of $60 million and milestone payments of $590 million.

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