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(Erlotinib)

Composition:

Each film-coated tablet contains 150mg erlotinib (as erlotinib hydrochloride)

ATC Code

L01XE03 (erlotinib)

Structure

Description

This compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.

Indication

Associated Conditions

Pharmacodynamics

Absortion.
Erlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%.The solubility of erlotinib is pH dependent. Solubility decreases pH increases. Smoking also decrease the exposure of erlotinib.

Peak Plasma Time: 4 hr

Volume of distribution.
Apparent volume of distribution = 232 L

Protein binding.
93% protein bound to albumin and alpha-1 acid glycoprotein (AAG)

Metabolism.
Metabolism occurs in the liver. In vitro assays of cytochrome P450 metabolism showed that erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1.

Hover over products below to view reaction partnerssss
Erlotinib
2-(4-(3-Ethynylanilino)-6-(2-methoxyethoxy)quinazolin-7-yl)oxyethanol

Excretion: Feces 83%; urine 8%

Half Life. Median half-life of 36.2 hours.

Clearance: 24% higher in smokers

Peak Plasma Time: 4 hr

Volume of distribution.
Apparent volume of distribution = 232 L

Protein binding.
93% protein bound to albumin and alpha-1 acid glycoprotein (AAG)

Metabolism.
Metabolism occurs in the liver. In vitro assays of cytochrome P450 metabolism showed that erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1.

Hover over products below to view reaction partnerssss
Erlotinib
2-(4-(3-Ethynylanilino)-6-(2-methoxyethoxy)quinazolin-7-yl)oxyethanol

Excretion: Feces 83%; urine 8%

Half Life. Median half-life of 36.2 hours.

Clearance: 24% higher in smokers

Mechanism of Action

The mechanism of clinical antitumor action of erlotinib is not fully characterized. Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibition with regard to other tyrosine kinase receptors has not been fully characterized. EGFR is expressed on the cell surface of normal cells and cancer cells.

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