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GDC-4198 + giredestrant
- Development stage
- Unknown
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
GDC-4198 + giredestrant is an oral, experimental combination therapy currently in early clinical development for the treatment of locally advanced or metastatic estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer in patients who have progressed on prior CDK4/6 inhibitor therapy. GDC-4198 is a new generation small molecule inhibitor targeting cyclin-dependent kinases 2, 4, and 6 (CDK2/4/6) developed by Regor Therapeutics and is classified as an antineoplastic agent. Giredestrant is a next-generation, oral selective estrogen receptor degrader (SERD) that antagonizes and degrades the estrogen receptor (ER). The combination is being assessed to overcome resistance to hormonal and CDK4/6 therapies by targeting both cell cycle regulation and hormone receptor signaling pathways[2][4][7][9].
- Other names
- GDC-4198 + giredestrant
02
Targets
ER (Estrogen receptor)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)
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