Dual-Targeting PSMA And FRα Drug Conjugate Advances to U.S. Trial for Prostate Cancer

MVB-101 (aka CBP-1018) is a new clinical-stage drug conjugate for prostate cancer simultaneously targets PSMA and folate receptor alpha (FRα) to overcome tumor heterogeneity. The drug is a bivalent peptide-like drug conjugate roughly one-fiftieth the size of a traditional antibody drug conjugate,designed to diffuse more rapidly into solid tumors. It delivers monomethyl auristatin E (MMAE), a tubulin inhibitor already used in several approved antibody drug conjugates, though no antibody drug conjugate has yet been approved for prostate cancer.

FRα is a deliberate choice because cancer cells rely heavily on folate receptors for folate uptake, and FRα is linked to core metabolism, making it less likely to be downregulated as an escape mechanism. Expression studies show FRα in a meaningful subset of prostate tumors, including those with low or heterogeneous PSMA.

The dual-targeting strategy covers a broader range of tumor cells. Up to 20% of circulating tumor cells can be PSMA-negative even when metastases show strong PSMA on imaging. By adding FRα, the drug can bind PSMA-low or PSMA-negative cells that are still FRα-positive, reducing the likelihood that a subpopulation escapes.

Early clinical data from a an ongoing Phase 1 study in China with 59 metastatic castration-resistant prostate cancer patients showed that MVB-101 is safe and well tolerated, with no dose-limiting toxicities or drug-related deaths. Median radiographic progression-free survival was 9.2 months in evaluable patients.

The program is advancing to a U.S. Phase 1b/2a trial expected to begin in the third quarter of 2026, evaluating a subgroup of prostate cancer patients, though details remain undisclosed.

Clinical trial.