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Letrozole

Indications and uses Pharmacokinetics Side effects
Letrozole
Letrozole structure
CAS No.
112809-51-5
Chemical Name:
Letrozole
Synonyms
Letroz;FEMARA;etrozoL;Lelrozol;Lerozole;LETROZOL;LETRAZOLE;CGS-20267;LETROZOLE;letrozolex
CBNumber:
CB9286355
Molecular Formula:
C17H11N5
Formula Weight:
285.3
MOL File:
112809-51-5.mol

Letrozole Properties

Melting point:
181-183°C
Boiling point:
563.5±60.0 °C(Predicted)
Density 
1.21±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: >50mg/mL
pka
1.52±0.11(Predicted)
form 
White powder
color 
white to off-white
Merck 
14,5450
InChIKey
HPJKCIUCZWXJDR-UHFFFAOYSA-N
CAS DataBase Reference
112809-51-5(CAS DataBase Reference)
FDA UNII
7LKK855W8I
NCI Dictionary of Cancer Terms
Femara; letrozole
NCI Drug Dictionary
Femara
ATC code
L02BG04
SAFETY
  • Risk and Safety Statements
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  26-36
WGK Germany  3
RTECS  DI4957000
HS Code  2933997500

Letrozole price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 182541 Aromatase Inhibitor II, Letrozole 112809-51-5 25mg $129 2021-03-22 Buy
Sigma-Aldrich Y0000685 Letrozole European Pharmacopoeia (EP) Reference Standard 112809-51-5 $190 2021-03-22 Buy
Sigma-Aldrich 1356971 Letrozole United States Pharmacopeia (USP) Reference Standard 112809-51-5 200mg $366 2021-03-22 Buy
Cayman Chemical 11568 Letrozole ≥98% 112809-51-5 10mg $35 2021-03-22 Buy
Cayman Chemical 11568 Letrozole ≥98% 112809-51-5 25mg $74 2021-03-22 Buy

Letrozole Chemical Properties,Uses,Production

Indications and uses

Letrozole 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.

Pharmacokinetics

Absorption of oral letrozole is rapid and complete and steady state is achieved in 2–6 weeks with administration of letrozole 2.5mg once daily. The major route of elimination of letrozole is via metabolism to a pharmacologically inactive carbinol metabolite. The cytochrome P450 (CYP) 3A4 and CYP2A6 isozymes metabolize letrozole to a pharmacologically inactive carbinol metabolite. Renal excretion of a glucuronide conjugate of the carbinol metabolite of letrozole represents the major route of drug clearance.

Side effects

Randomized 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.

Description

Letrozole (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 Properties

white to light yellow crystal

Originator

Novartis (Switzerland)

Uses

A nonsteroidal aromatase inhibitor structurally related to Fadrozole. Antineoplastic

Manufacturing Process

From 4-bromomethylbenzonitrile and 1H-[1,2,4]triazole was obtained 4- [1,2,4]triazol-1-ylmethylbenzonitrile. Treatment of that with strong base (tertBuOK) results in formation of the anion by removal of the relatively acidic benzyl proton. This anion was condensed with p-fluorobenzinitrile to give benzhydryl tetrazole (Letrozole)

brand name

Femara (Novar tis).

Therapeutic Function

Antineoplastic

General Description

Letrozole, 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.

Mechanism of action

Inhibition of arom atase by letrazole is competitive and highly specific , with no effect on enzymes that are responsible for the production of glucocorticosteroids and mineralocorticosteroids. This agent is significantly more effective than tamoxifen in treating horm one-dependent cancer.

Clinical Use

Femara 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.

References

https://www.drugbank.ca/drugs/DB01006
https://en.wikipedia.org/wiki/Letrozole

Letrozole Preparation Products And Raw materials

Raw materials

Preparation Products


Letrozole Suppliers

Global( 454)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Guangzhou TongYi biochemistry technology Co.,LTD
+8613073028829
mack@tongyon.com China 3001 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 420 58
Hebei Bonster Technology Co.,Limited
+86-13315996897
0086-13315996897 Wendy@bsterltd.com CHINA 998 58
WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
15327141851 027-81302090
027-81302088 2851686515@qq.com CHINA 280 58
WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
18007166089 86-18007166089
circlepowder01@gmail.com CHINA 230 58
Qingdao kaimoshi biochemical technology co., ltd.
+(86) 571 87700752
+(86) 571 87700752 info@kaimosi.com CHINA 145 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
13588875226 86-571-88216897、88216896
86-571-88216895 sales@hzclap.com CHINA 6469 58
Handan Tongyi New Material Technology Co., Ltd
+8617330042575
ty003@handantongyi.com CHINA 339 58
Hebei Ruiyao Biotechnology Co. Ltd
15532235888 15632182983
031188180881 admin@ruiyaobio.com CHINA 846 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55

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View Lastest Price from Letrozole manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-12-01 Letrozole
112809-51-5
US $10.00 / KG 1KG 99.99% 500kg/month Handan Tongyi New Material Technology Co., Ltd
2021-12-01 Letrozole
US $0.00 / KG 100g 98%+ 100kg WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
2021-12-01 Letrozole
112809-51-5
US $1024.00 / KG 100g 98%+ 100kg WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD

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