Drug intelligence / Profile preview

XL102 + abiraterone + prednisone

Development stage
Discontinued
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

XL102 + abiraterone + prednisone is an investigational **multi-drug combination** under clinical evaluation for the treatment of prostate cancer. - **XL102** is an oral, potent and selective small molecule inhibitor of cyclin-dependent kinase 7 (**CDK7**), which regulates cell cycle and transcriptional activity critical for cancer growth. - **Abiraterone** is a small molecule, selective and irreversible inhibitor of steroid 17α-hydroxylase/17,20-lyase (**CYP17A1**), blocking androgen biosynthesis, and is approved for use in metastatic castration-resistant and metastatic high-risk castration-sensitive prostate cancer when combined with prednisone[1][2][3][7]. - **Prednisone** is a synthetic glucocorticoid (corticosteroid) that is co-administered to mitigate the mineralocorticoid excess and cortisol suppression that arise from CYP17A1 inhibition by abiraterone[1][2][3][7]. This combination is being explored for enhanced antitumor efficacy in prostate cancer due to targeting both transcriptional activity (via CDK7) and androgen production (via CYP17A1), supplemented by glucocorticoid support to manage side effects.

02

Targets

CDK7CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GR (Glucocorticoid receptor)

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