tacaciclib

XL102 (tacaciclib) is a potent, selective, and orally bioavailable small molecule inhibitor of cyclin-dependent kinase 7 (CDK7), a key regulator of cellular transcriptional and cell cycle machinery. CDK7 controls cell cycle progression by phosphorylating other cyclin-dependent kinases (CDKs 1, 2, 4, and 6) and regulates transcription through phosphorylation of RNA polymerase II. Overexpression of CDK7 has been observed in multiple cancers such as breast cancer (including hormone receptor-positive and triple-negative subtypes), prostate cancer (including metastatic castration-resistant disease), and ovarian cancer. Preclinical studies have shown that XL102 induces anti-proliferative activity and cell death in various cancer cell lines as well as tumor regression in xenograft models. The drug is being developed for advanced or metastatic solid tumors with ongoing phase 1 clinical trials evaluating its safety both as monotherapy and in combination regimens[1][2][3][4][5][6][7].

Other names

tacaciclibXL102XL-102XL 102AUR102AUR-102AUR 102