ChemicalBook > Product Catalog > API > Antineoplastic agents > Hormonal antineoplastic drugs > Letrozole
- Product Name:Letrozole
- Synonyms: Aromatase Inhibitor II, Letrozole - CAS 112809-51-5 - Calbiochem LetrozoleUsp28 Letrozole99% CGS-20267, Femara LETRAZOLE letrozolex 4,4'-(1H-1,2,4-Triazol-1-ylmethylene)dibenzonitrile 4,4'-(1H-1,2,4-Triazole-1-ylmethylene)bisbenzonitrile
- Product Categories: - Anti-Cancer Pharmaceutical material and intermeidates Active Pharmaceutical Ingredients Letrozole Antineoplastic Pharmaceuticals API's APIs Antibiotics All Inhibitors anti-neoplastic Inhibitors Intermediates & Fine Chemicals Aromatics Heterocycles ELOXATIN Anti-cancer&immunity
- Mol File:112809-51-5.mol
Letrozole Chemical Properties
- Melting point:181-183°C
- storage temp. -20°C Freezer
- solubility DMSO: >50mg/mL
- form White powder
- color white to off-white
- Merck 14,5450
- CAS DataBase Reference112809-51-5(CAS DataBase Reference)
Letrozole Usage And Synthesis
- Indications and usesLetrozole is part of a new generation of highly selective aromatase inhibitors and is an artificially synthesized benzotriazole derivative. Letrozole inhibits aromatase to lower estrogen levels, thus preventing estrogen from stimulating tumor growth. Its in vivo activity is 150-250 times stronger than that of first generation aromatase inhibitor Amarante. As it is highly selective, it will not impact glucocorticoid, mineralocorticoid and thyroid functions; even at high dosages, it will not have any inhibiting effects on adrenal corticosteroid secretion, giving it a high treatment index. Letrozole has no latent toxicity towards any bodily systems and target organs, has no mutagenicity and carcinogenic effects, has minimal toxic side effects, is well-tolerated, and has stronger anticancer effects than other aromatase inhibitors and antiestrogen drugs. Letrozole is suitable for advanced breast cancer postmenopausal patients who have not responded to estrogen-suppressing treatment and for early breast cancer treatment. It is used to treat postmenopausal patients with advanced breast cancer and serves as a second-line treatment to follow unsuccessful antiestrogen treatment. Compared to the current standard Tamoxifen treatment, Letrozole can better prevent the risk of breast cancer recurrence.
- Side effectsRandomized grouping studies have shown that daily oral ingestion of 2.5mg Letrozole leads to a 33% rate of drug-related negative reactions, a percentage much lower than AG group’s 46%. Negative reactions to Letrozole are mostly mild or moderate, consisting mostly of nausea (2-9%), headache (0-7%), bone pain (4-10%), hot flashes (0-9%) and weight gain (2-8%). Other uncommon side effects include constipation, diarrhea, itching, rash, joint pain, chest pain, abdominal pain, fatigue, insomnia, dizziness, edema, high blood pressure, arrhythmia, thrombosis, dyspnea, vaginal bleeding, etc.
- DescriptionLetrozole (trade name: Femara) is an orally active nonsteroidal aromatase inhibitor. As a competitive inhibitor of the aromatase, Letrozole inhibits the conversion of androgens to estrogen (estrogen stimulates breast tissues and breast cancer reoccurrence) and gonadal steroidogenesis. It can be used for the treatment of breast cancer that is hormonally-responsive or has an unknown receptor status in postmenopausal women. Besides this, Letrozole also has some off-label use such as ovarian stimulation, pretreatment of termination of pregnancy, treatment of gynecomastia, treatment of endometriosis, and promoting spermatogenesis for male patients of nonobstructive azoospermia.
- Chemical Propertieswhite to light yellow crystal
- OriginatorNovartis (Switzerland)
- UsesA nonsteroidal aromatase inhibitor structurally related to Fadrozole. Antineoplastic
- brand nameFemara (Novar tis).
- General DescriptionLetrozole, 4,4'-(1H-1,2,4-triazol-1-ylmethylene)dibenzonitrile (Femara), is used for most of thesame indications as anastrozole. It reduces concentrations ofestrogens by 75% to 95%, with maximal suppressionachieved within 2 to 3 days. Letrozole is specific for aromataseinhibition, with no additional effects on adrenal corticoidbiosynthesis. CYPs 3A4 and 2A6 are involved in themetabolism of letrozole to the major carbinol metabolite,which is inactive. The loss of the triazole ring, which is involvedin coordination of the heme iron, would explain theloss of activity. Letrozole strongly inhibits CYP2A6 invitro, with moderate inhibition of CYP2C19. The effect ofthis in vitro inhibition on the pharmacokinetics of coadministereddrugs is unknown. Tamoxifen reduces the levels ofletrozole significantly if they are used together, so combinationtreatment with these agents is not recommended.
- Clinical UseFemara was launched in France and the UK for second-line treatment of advanced breast cancer. Letrazole can be synthesized in two steps from 4- bromomethyl-benzonitrile with 1,2,4-triazole and is a third generation aromatase inhibitor. It is a highly specific inhibitor of P450arom which prevents the conversion of androstenedione to estrone. The reduction of plasma estrogen was immediate and long lasting. This is accomplished with no inhibition of other steroid biosynthesis making it the most selective aromatase inhibitor tested. Letrazole has remarkable antitumor activity, is well tolerated and has no toxic side effects. It is 10,000 times more potent than aminoglutethimide, in vivo, the first well established aromatase inhibitor.
Letrozole Preparation Products And Raw materials
- [1-Hydroxy-3-(methylpentylamino)-propylidene]bisphosphonic acid sodium salt Irinotecan hydrochloride trihydrate 4,4''-DICYANOBENZOPHENONE(INTERMEDIATE OF LETROZOLE ) 4-[α-(4-Cyanophenyl)-hydroxymethyl]-benzonitrile ( For Letrozole ) 5-Methyl-1,3-benzenediacetonitrile 4-BENZYLBENZONITRILE 4,4'-(1-METHYLENE) BIS-BENZONITRILE 1-BENZHYDRYL-1,2,4-TRIAZOLE (S)-1-(4-CYANOPHENYL)ETHANAMINE 1,1-bis(4-methylphenyl)methanamine (R)-1-(4-CYANOPHENYL)ETHANAMINE 4-((1H-1,2,4-triazol-1-yl)methyl)benzonitrile (intermediate of letrozole),INTERMEDIATE OF LETROZOLE,4-[1-(1,2,4-triazolyl)-methyl]-benzonitrile ( For Letrozole ) 4-Cyanobenzylamine Letrozole 5-Methyl-1H-benzotriazole Chlorodimethylphenylsilane Tolyltriazole 1,2,4-Triazole
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