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TY-302 + tamoxifen
- Development stage
- Unknown
- Lead developer
- TYK Medicines
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
TY-302 + tamoxifen is a combination therapy comprising TY-302, a potent and selective oral cyclin-dependent kinase 4/6 (CDK4/6) inhibitor, and tamoxifen, a selective estrogen receptor modulator (SERM). TY-302 is developed by TYK Medicines and targets CDK4/6 to inhibit retinoblastoma protein (Rb) phosphorylation, arresting the cell cycle at the G1 phase and inhibiting tumor cell proliferation. Tamoxifen antagonizes the estrogen receptor, blocking proliferative signals in hormone-responsive breast cancers. This combination is under clinical evaluation for the treatment of estrogen receptor (ER) positive, human epidermal growth factor receptor 2 (HER2) negative advanced breast cancer. The strategy leverages dual blockade of cyclin-dependent kinases and hormone signaling to overcome resistance and improve clinical outcomes in HR+/HER2- breast cancer patients[1][5][7].
- Other names
- TY-302 + tamoxifen
02
Targets
ABCB1 (P-glycoprotein)CDK6 (Cyclin-dependent kinase 6)LSR (Lipolysis-stimulated lipoprotein receptor)CDK4 (Cyclin-dependent kinase 4)MRP (Multidrug resistance-associated protein family)ER (Estrogen receptor)
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