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larotrectinib
- Development stage
- Approved
- Lead developer
- Eli Lilly
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Larotrectinib is an orally administered small molecule tyrosine kinase inhibitor developed to treat adult and pediatric patients with solid tumors that harbor neurotrophic receptor tyrosine kinase (NTRK) gene fusions. These fusions lead to constitutive activation of tropomyosin receptor kinases (Trk), which drive tumor growth and survival. Larotrectinib selectively inhibits TRK proteins—including TRKA, TRKB, and TRKC—encoded by the NTRK1, NTRK2, and NTRK3 genes. By blocking these kinases, larotrectinib disrupts oncogenic signaling pathways in cancer cells with NTRK gene fusions, resulting in inhibition of cell proliferation and induction of apoptosis. It is indicated for use when tumors are metastatic or unresectable or when no satisfactory alternative treatments exist.
- Brand names
- Vitrakvi
- Other names
- larotrectinibLOXO-101LOXO101LOXO 101Vitrakvi
02
Targets
NTRK3 (Tropomyosin receptor kinase C)TNK2 (Activated Cdc42-associated kinase 1)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK1 (Tropomyosin-related receptor kinase A)
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