Phase 1 relative bioavailability study of tepotinib
Research type
Research Study
Full title
A Phase 1, Open-label, Randomized, Cross-over Trial to Investigate the Relative Bioavailability of Two Tepotinib Film-Coated Tablet Formulations in Healthy Volunteers
IRAS ID
192109
Contact name
Salvatore Febbraro
Contact email
Sponsor organisation
Merck KGaA
Eudract number
2015-004369-95
Duration of Study in the UK
0 years, 2 months, 0 days
Research summary
Despite significant progress in the early detection, diagnosis, and treatment of tumors, such as lung and breast tumors, the effectiveness of most cancer treatments remains unsatisfactory. Tumors that are initially responsive to treatment develop resistance over time; and a number of tumors, do not respond to currently available treatments. 5-year patient survival is < 5%.
The resistance of certain tumors to conventional standard treatment for cancer (Chemotherapy) has been linked to their genetic complexity; however recent findings have shown that many solid tumors are “addicted” to particular activated kinases (a receptor which is a substance produced by the body to assist in a chemical reaction that regulates proteins in the body). Targeting such kinases with drugs that block the pathway for tumor growth represents a promising anticancer approach.
c-Met is a type of kinase that is bound together by hepatocyte growth factor (HGF). This complex (HCF bound to c-Met) has been seen to be present in tumor progression, and as such there is an increasing interest to target this to stop tumor growth. Previous studies targeting the c-Met kinase receptor have been performed to prove this concept.
In non-clinical studies tepotinib has been shown to block the c-Met receptor kinase and growth pathway in tumors. Tepotinib has previously been tested in humans, it has been shown to be generally well tolerated.
This study is to investigate the amount of tepotinib that reaches the blood using a new Phase 3 film-coated tablet formulation (1 x 500mg tablet) of tepotinib compared to the current Phase 2 film coated tablet formulation (5 x 100mg tablets). Due to formulation changes (new excipients and different compaction) between the forthcoming Phase 3 and the current Phase 2 film-coated tablet formulation. This study is being performed prior to Phase 3, to bridge clinical results from Phase 2 trials and to potentially adjust the dose.
REC name
Wales REC 2
REC reference
15/WA/0362
Date of REC Opinion
3 Dec 2015
REC opinion
Further Information Favourable Opinion