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Brivanib alaninate for cancer
Ivan Diaz-Padilla1, Lillian L Siu
1Princess Margaret Hospital, Toronto, Ontario, M5G2M9 Canada. lillian.siu@uhn.on.ca
Introduction:
Angiogenesis inhibition represents a rational therapeutic strategy in the management of solid tumors. Brivanib is a dual tyrosine kinase inhibitor with selectivity against VEFGR-2 and FGFR.
Areas Covered:
This review provides an updated summary of preclinical and clinical experience with brivanib in cancer. Data presented in abstract form from international conferences or journal articles found with a PubMed search of published literature up to December 2010 are described in this review.
Expert Opinion:
Brivanib appears tolerable and exhibits favorable pharmacokinetic and pharmacodynamic profiles with evidence of target inhibition in surrogate tissues. Clinical and pharmacodynamic data support an oral once daily administration at 800 mg. Brivanib shows promising activity as single agent in hepatocellular carcinoma and in combination with cetuximab in colorectal cancer. Further evaluations with cytotoxic chemotherapy and in other solid tumors are currently ongoing.
Insights
Brivanib, a dual tyrosine kinase inhibitor, shows tolerable safety and promising efficacy in treating hepatocellular carcinoma and colorectal cancer. Further studies are ongoing to evaluate its potential in other solid tumors and combinations.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Angiogenesis inhibition is a key strategy for solid tumor treatment.
- Brivanib is a dual tyrosine kinase inhibitor targeting VEGFR-2 and FGFR.
Purpose of the Study:
- To review preclinical and clinical data of brivanib in cancer treatment.
- To summarize brivanib's safety, efficacy, and pharmacokinetic/pharmacodynamic profiles.
Main Methods:
- Literature review of published data up to December 2010.
- Analysis of preclinical and clinical trial results presented in abstracts and journals.
Main Results:
- Brivanib demonstrates a tolerable safety profile and favorable pharmacokinetics.
- Evidence of target inhibition in surrogate tissues supports brivanib's mechanism.
- Oral administration of 800 mg once daily is supported by clinical data.
Conclusions:
- Brivanib shows promise as a single agent in hepatocellular carcinoma.
- Combination therapy with cetuximab demonstrates activity in colorectal cancer.
- Ongoing trials are exploring brivanib with chemotherapy and in other solid tumors.
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