{"entity":{"id":"arpi","kind":"term","name":"Androgen receptor pathway inhibitor (ARPI)","aka":["ARPI","ARPIs","ARSI","androgen receptor signalling inhibitor","androgen receptor pathway inhibitor","novel hormonal agent","NHA","next-generation antiandrogen","second-generation antiandrogen","AR antagonist","AR inhibitor","antiandrogen","anti-androgen","AR-V7","AR-targeted","AR antagonists"],"tldr":"The newer prostate cancer hormone pills (abiraterone, enzalutamide, apalutamide, darolutamide) that block the androgen receptor or the last steps of androgen production, used on top of standard testosterone suppression.","summary":"Abiraterone blocks CYP17 androgen synthesis (given with prednisone); enzalutamide, apalutamide and darolutamide are potent AR antagonists. Adding an ARPI to ADT extends survival in metastatic hormone-sensitive disease (LATITUDE, ARCHES, TITAN, ARASENS), in non-metastatic castration-resistant disease and in castration-resistant disease before or after docetaxel. Resistance arises via AR amplification, ligand-binding domain mutations, the AR-V7 splice variant and lineage plasticity to neuroendocrine disease; switching ARPIs after failure gives little benefit, so PSMA radioligands, PARP inhibitors and chemotherapy follow. Older antiandrogens (bicalutamide) are weaker first-generation drugs.","asOf":"2026-09-09","wikipedia":"https://en.wikipedia.org/wiki/Antiandrogen","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Antiandrogen"}],"tags":[],"related":[],"indications":["prostate"],"sections":[],"technologies":[],"targets":[],"drugs":["abiraterone","enzalutamide"],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"category":"Treatment jargon"},"route":"/terms/arpi/","neighbours":{"indication":[{"id":"prostate","kind":"indication","name":"Prostate cancer","route":"/indications/prostate/"}],"drug":[{"id":"abiraterone","kind":"drug","name":"Abiraterone acetate","route":"/drugs/abiraterone/"},{"id":"enzalutamide","kind":"drug","name":"Enzalutamide","route":"/drugs/enzalutamide/"}],"term":[{"id":"mcrpc-mhspc","kind":"term","name":"mCRPC and mHSPC (castration-resistant vs hormone-sensitive prostate cancer)","route":"/terms/mcrpc-mhspc/"}],"pairing":[{"id":"radium223-abiraterone-caution","kind":"pairing","name":"Radium-223 with abiraterone: a caution, not a combination","route":"/pairings/radium223-abiraterone-caution/"}],"paper":[{"id":"paper-psmafore-lancet-2024","kind":"paper","name":"PSMAfore: 177Lu-PSMA-617 versus a change of androgen receptor pathway inhibitor in taxane-naive mCRPC","route":"/key-papers/paper-psmafore-lancet-2024/"}]}}