Drug intelligence / Profile preview

bicalutamide + tremelimumab

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Bicalutamide is a nonsteroidal antiandrogen used primarily in the treatment of metastatic prostate cancer. It works by competitively inhibiting androgen receptors, thereby blocking the action of androgens (such as testosterone) that stimulate the growth of normal and malignant prostatic tissue[1][4][8]. Tremelimumab is a fully human IgG2 monoclonal antibody that targets cytotoxic T lymphocyte-associated antigen 4 (CTLA-4), an immune checkpoint receptor on activated T cells. By binding to CTLA-4, tremelimumab blocks its inhibitory effect on T cell activation, thereby enhancing immune-mediated tumor cell killing[5][6]. Tremelimumab is approved for use in combination with durvalumab for unresectable hepatocellular carcinoma and certain types of metastatic non-small cell lung cancer[2][5][6]. The combination of bicalutamide and tremelimumab represents a multi-modal approach targeting both hormonal pathways (androgen blockade) and immune checkpoints.

02

Targets

AR (Adrenergic receptors)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)

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