XL102 + fulvestrant

**XL102 + fulvestrant** is an investigational combination therapy in clinical trials for advanced solid tumors, including hormone receptor-positive breast cancer. XL102 is an orally bioavailable, selective, covalent small molecule inhibitor of cyclin-dependent kinase 7 (CDK7), developed as a targeted antineoplastic agent. CDK7 plays a critical role in the regulation of cell cycle progression and transcription by phosphorylating various CDKs and RNA polymerase II. By inhibiting CDK7, XL102 disrupts transcription and cell division, leading to cell cycle arrest and apoptosis in cancer cells[1][2][4]. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds and accelerates the degradation of the estrogen receptor, antagonizing estrogen-mediated signaling critical for the growth of hormone receptor-positive breast cancer[5]. The combination aims to target both transcriptional dependence and hormonal signaling in cancer, particularly in patients who are refractory to standard therapies[1].

Other names

XL102 + fulvestrant