abiraterone acetate + AZD8186

Abiraterone acetate is an oral small molecule prodrug of abiraterone, which inhibits the enzyme Cytochrome P450 17A1 (CYP17A1) (17α-hydroxylase/17,20 lyase), a key enzyme in androgen biosynthesis. By blocking CYP17A1, it reduces androgen production from the testes, adrenal glands, and prostate tumor tissue, leading to decreased levels of testosterone and other androgens that can drive prostate cancer progression[6][8]. It is primarily used in combination with prednisone for metastatic castration-resistant prostate cancer[1][4][8]. AZD8186 is an investigational oral small molecule inhibitor that selectively targets Phosphoinositide 3-kinase beta isoform (PI3Kβ). It has shown preclinical activity particularly in PTEN-deficient tumors. In clinical studies, AZD8186 has been evaluated both as monotherapy and in combination with antiandrogens such as abiraterone acetate for advanced solid tumors including prostate cancer[2][5]. The rationale for combining these agents is based on evidence that dual inhibition of androgen receptor signaling (by abiraterone) and PI3Kβ signaling (by AZD8186) may provide additive or synergistic antitumor effects in certain molecular subtypes such as PTEN-null cancers[2].

Brand names

Yonsa

Other names

abirateroneabiraterone acetate + AZD8186