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ceritinib + trametinib
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Ceritinib + trametinib is a combination of two small molecule targeted therapies used in clinical trials for cancer treatment. Ceritinib is an oral anaplastic lymphoma kinase (ALK) and ROS1 tyrosine kinase inhibitor that blocks signaling pathways involved in tumor cell proliferation and survival. Trametinib is a MEK inhibitor that targets the mitogen-activated protein kinase (MAPK) pathway by inhibiting MEK1 and MEK2 enzymes. The rationale for combining these agents stems from preclinical evidence suggesting that dual inhibition of ALK/ROS1 and MEK can overcome resistance to ALK inhibitors in non-small cell lung cancer (NSCLC). This combination has been studied primarily in patients with advanced or refractory NSCLC harboring ALK or ROS1 rearrangements, as well as metastatic melanoma. Clinical studies have shown manageable toxicity profiles with common adverse events including diarrhea, rash, abdominal pain, and elevated liver enzymes[1][3][5]. The combination aims to improve outcomes after progression on prior targeted therapies.
- Other names
- ceritinib + trametinib
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)ENTPD1 (Ectonucleoside triphosphate diphosphohydrolase 1)
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