Gridegalutamide is an investigational oral androgen receptor (AR) degrader being developed for the treatment of

metastatic castration-resistant prostate cancer Prostate cancer is the neoplasm, uncontrolled growth of cells in the prostate, a gland in the male reproductive system below the bladder. Abnormal growth of the prostate tissue is usually detected through Screening (medicine), screening tests, ...

(mCRPC). It belongs to a class of drugs called proteolysis targeting chimeras (PROTACs), which are designed to selectively degrade specific proteins by hijacking the

ubiquitin-proteasome system Proteasomes are essential protein complexes responsible for the degradation of proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that help such reactions are called proteases. Proteasomes are found inside all e ...

. CC-94676 employs a unique dual mechanism of action, combining AR degradation with AR antagonism, potentially offering advantages over traditional AR inhibitors in overcoming resistance mechanisms. Initially developed by

Celgene Celgene Corporation, headquartered in Summit, New Jersey, was a pharmaceutical company that produced cancer and immunology drugs. Its primary products were Revlimid (lenalidomide), which is used in the treatment of multiple myeloma (63% of 2018 r ...

and now under

Bristol Myers Squibb The Bristol-Myers Squibb Company, Trade name, doing business as Bristol Myers Squibb (BMS), is an American multinational pharmaceutical company. Headquartered in Princeton, New Jersey, BMS is one of the world's largest pharmaceutical companies ...

, CC-94676 has demonstrated AR protein degradation and suppression of tumor growth in CRPC mouse models. As of 2024, CC-94676 is being evaluated in phase I clinical trials for patients with mCRPC who have progressed on

androgen deprivation therapy Androgen deprivation therapy (ADT), also called androgen ablation therapy or androgen suppression therapy, is an antihormone therapy whose main use is in treating prostate cancer. Prostate cancer cells usually require androgen, androgen hormones, ...

and at least one prior secondary hormonal therapy.

References

{{antineoplastic-drug-stub Acetanilides Benzonitriles Trifluoromethyl compounds Piperidines Nitriles Imidazolidinones Piperazines