Olmutinib
Olmutinib Uses, Dosage, Side Effects, Food Interaction and all others data.
Olmutinib is an orally active epidermal growth factor receptor inhibitor used in the treatment of T790M mutation positive non-small cell lung cancer. It is available under the brand name Olita made by Hanmi Pharmaceuticals . Olmutinib was developed by Hanmi Pharmaceuticals and Boehringer Ingelheim. Olmutinib recieved breakthrough therapy designation in the United States in December 2015 and was approved for use in Korea in May 2016.
Olmutinib selectively and irreversibly binds and inhibits epidermal growth factor receptors (EGFR) with the T790M activating mutation. EGFRs are frequently over-expressed in lung cancer and contribute to activation of the phosphoinositide 3-kinase and mitogen activated protein kinase pathways which both promote cell survival and proliferation . By inhibiting EGFR activation, olmutinib attenuates the activation of these tumor promoting pathways.
Trade Name | Olmutinib |
Generic | Olmutinib |
Olmutinib Other Names | Olmutinib |
Type | |
Formula | C26H26N6O2S |
Weight | Average: 486.59 Monoisotopic: 486.183795275 |
Protein binding | Data not yet available. |
Groups | Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
For use in treatment of metastatic T790M mutation positive non-small cell lung cancer .
How Olmutinib works
Olmutinib covalently binds a cysteine residue near the kinase domain of mutant EGFRs to prevent phosphorylation of the receptor . This inhibits receptor signalling as phosphorylation is necessary for recruitment of signalling cascade proteins.
Toxicity
No toxicological investigation has been completed.
Volume of Distribution
Data not yet available.
Elimination Route
tmax of 3-4h with oral administration .
Half Life
8-11h .
Clearance
Data not yet available.
Elimination Route
Data not yet available.
Innovators Monograph
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