Erlotinib
- CAS NO.:183321-74-6
- Empirical Formula: C22H23N3O4
- Molecular Weight: 393.44
- MDL number: MFCD02089651
- EINECS: 689-196-2
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-05-22 11:16:15
What is Erlotinib?
Absorption
Erlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%. Peak plasma levels occur 4 hours after dosing. The solubility of erlotinib is pH dependent. Solubility decreases pH increases. Smoking also decrease the exposure of erlotinib.
Toxicity
Symptoms of overdose include diarrhea, rash, and liver transaminase elevation. The most common adverse reactions (>50%) in NSCLC are rash, diarrhea, anorexia and fatigue. The most common adverse reactions (>50%) in pancreatic cancer are fatigue, rash, nausea and anorexia.
Description
Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-
The Uses of Erlotinib
Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.
Indications
Erlotinib is indicated for:
The safety and efficacy of erlotinib have not been established for patients with NSCLC whose tumors show other EGFR mutations. Additionally it is not recommended for use in combination with platinum-based chemotherapy.
What are the applications of Application
Erlotinib, Free Base is a tyrosine kinase inhibitor
Background
Erlotinib is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase that is used in the treatment of non-small cell lung cancer, pancreatic cancer and several other types of cancer. It is typically marketed under the trade name Tarceva. Erlotinib binds to the epidermal growth factor receptor (EGFR) tyrosine kinase in a reversible fashion at the adenosine triphosphate (ATP) binding site of the receptor. Recent studies demonstrate that erlotinib is also a potent inhibitor of JAK2V617F, which is a mutant form of tyrosine kinase JAK2 found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. This finding introduces the potential use of erlotinib in the treatment of JAK2V617F-positive PV and other myeloproliferative disorders.
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.
Properties of Erlotinib
Melting point: | 159-160 °C |
Boiling point: | 553.6±50.0 °C(Predicted) |
Density | 1.24 |
storage temp. | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
solubility | Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly) |
form | Solid |
color | White |
Safety information for Erlotinib
Signal word | Danger |
Pictogram(s) |
Health Hazard GHS08 |
GHS Hazard Statements |
H227:Flammable liquids H304:Aspiration hazard H350:Carcinogenicity |
Precautionary Statement Codes |
P201:Obtain special instructions before use. P202:Do not handle until all safety precautions have been read and understood. P210:Keep away from heat/sparks/open flames/hot surfaces. — No smoking. P280:Wear protective gloves/protective clothing/eye protection/face protection. P331:Do NOT induce vomiting. P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. P308+P313:IF exposed or concerned: Get medical advice/attention. P370+P378:In case of fire: Use … for extinction. P405:Store locked up. P403+P235:Store in a well-ventilated place. Keep cool. |
Computed Descriptors for Erlotinib
Abamectin manufacturer
Jigs Chemical ltd
Sakar Healthcare
Shreyaa Medilife Private Limited
Aspen Biopharma Labs Pvt Ltd
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