Erlotinib

Bezeichnung:Erlotinib

CAS-Nr183321-74-6

Englisch Name:Erlotinib

CBNumberCB9285914

SummenformelC22H23N3O4

Molgewicht393.44

MOL-Datei183321-74-6.mol

Erlotinib physikalisch-chemischer Eigenschaften

Schmelzpunkt	159-160 °C
Siedepunkt	553.6±50.0 °C(Predicted)
Dichte	1.24
storage temp.	Keep in dark place,Sealed in dry,Store in freezer, under -20°C
Löslichkeit	Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
pka	5.32±0.30(Predicted)
Farbe	White
CAS Datenbank	183321-74-6(CAS DataBase Reference)

Sicherheit

S-Sätze:	24/25
HS Code	29335990
Giftige Stoffe Daten	183321-74-6(Hazardous Substances Data)

Gefahreninformationscode (GHS)

Erlotinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC₅₀ = 2.5 μM). This inhibits tumor growth in human head and neck carcinoma HN5 tumor xenografts in mice with an ED₅₀ value of 9 mg/kg. Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC₅₀ = 4.6 μM) and JAK2 mutant JAK2^V617F positive hematopoietic progenitor cells (IC₅₀ = 5 μM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia. Formulations containing erlotinib have been used to treat certain forms of cancer, including non-small cell lung cancer.
Verwenden
Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.
Verwenden
A tyrosine kinase inhibitor
Verwenden
antineoplastic;tyrosine kinase inhibitor
Definition
ChEBI: A quinazoline compound having a (3-ethynylphenyl)amino group at the 4-position and two 2-methoxyethoxy groups at the 6- and 7-positions.
Trademarks
Tarceva (OSI).
Allgemeine Beschreibung
Class: receptor tyrosine kinase
Treatment: NSCLC
Oral bioavailability = 60%
Elimination half-life = 36 h
Protein binding = 93%
Clinical Use
Erlotinib
Treatment of locally advanced or metastatic nonsmall cell lung cancer after failure of at least 1 other regime
Pancreatic cancer
Nebenwirkungen
- Burning, tingling, numbness or pain in the hands, arms, feet, or legs.
- cough or hoarseness.
- diarrhea (severe)
- difficult or labored breathing.
- fever or chills.
- rash (severe)
- sensation of pins and needles.
- stabbing chest pain.
Synthese
The synthesis of Erlotinib is as follows:
N-dimethylformamidine, 0.72 g (6.15 mmol) of N '- [2-cyano-4,5-bis (2-methoxyethoxy) phenyl] ) Of 3-aminophenylacetylene and 8 mL of acetic acid were reacted in a 50 mL reaction flask at 125 ° C for 1 hour and cooled to room temperature.20 mL of ice water was added to the mixture, the pH was adjusted to 10 with aqueous ammonia, and the mixture was stirred for 1 hour, suction filtered and the filter cake washed with water until neutral.The filter cake was dried to obtain 2.15 g of erlotinib in a yield of 91.5%.
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs Analgesics: increased risk of bleeding with NSAIDs.
Antacids: concentration possibly reduced by antacids, give at least 4 hours before or 2 hours after erlotinib.
Anticoagulants: increased risk of bleeding with coumarins
Antipsychotics: avoid concomitant use with clozapine, increased risk of agranulocytosis.
Antivirals: avoid with boceprevir.
Ulcer-healing drugs: avoid with cimetidine, esomeprazole, famotidine, lansoprazole, nizatidine, pantoprazole and rabeprazole; concentration reduced by ranitidine, give at least 2 hours before or 10 hours after ranitidine; concentration reduced by omeprazole - avoid.
Stoffwechsel
Erlotinib is metabolised mainly by the cytochrome P450 isoenzyme CYP3A4, and to a lesser extent by CYP1A2. Extrahepatic metabolism by CYP3A4 in intestine, CYP1A1 in lung, and 1B1 in tumour tissue potentially contribute to the metabolic clearance of erlotinib.
Metabolic pathways include demethylation, to metabolites OSI-420 and OSI-413, oxidation, and aromatic hydroxylation. The metabolites OSI-420 and OSI-413 have comparable potency to erlotinib in non-clinical in vitro assays and in vivo tumour models. They are present in plasma at levels that are <10 % of erlotinib and display similar pharmacokinetics as erlotinib. Erlotinib is excreted predominantly as metabolites via the faeces (>90%) with renal elimination accounting for only a small amount (approximately 9%) of an oral dose. Less than 2% of the orally administered dose is excreted as parent substance

Erlotinib Upstream-Materialien And Downstream Produkte

Erlotinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

183321-74-6, Erlotinib Verwandte Suche:

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