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XP-102 + trametinib
- Development stage
- Unknown
- Lead developer
- Xynomic Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**XP-102 + trametinib** is an investigational combination therapy under clinical evaluation for advanced malignant solid tumors (including melanoma, colorectal cancer, non-small-cell lung cancer, and thyroid cancer) that harbor BRAF V600 mutations. XP-102 is a novel small molecule BRAF inhibitor, while trametinib is an approved MEK1/2 inhibitor marketed as Mekinist. The rationale for combination is to achieve more potent blockade of the MAPK pathway, which is commonly reactivated as resistance to single-agent BRAF inhibition. XP-102 is being developed and tested both as monotherapy and in combination with trametinib in a multicenter phase 1/2 (ENHANCE, NCT05275374) study in patients with BRAF V600-mutant advanced solid tumors[1][3][5][7].
- Other names
- XP-102 and XP-102 in combination with trametinibXP102 and XP-102 in combination with trametinibXP 102 and XP-102 in combination with trametinibXP-102 plus trametinibXP102 plus trametinibXP 102 plus trametinib
02
Targets
RAF1 (c-Raf-1 (Y340D/Y341D))BRAF (B-Raf proto-oncogene, serine/threonine kinase)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)
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