Product Name

Ketoconazole

Name: Ketoconazole - LGM Pharma
SKU: 65277-42-1

CAS Number

65277-42-1

LGM Pharma is an API distributor. LGM Pharma can supply CGMP and/or DMF products, subject to availability and manufacturer requirements. LGM Pharma does not sell or supply APIs or finished dosage products to individual patients, doctors, pharmacies, or any pharmaceutical companies.

Questions? Call our customer API support number 1-(800)-881-8210

Product Name:

Ketoconazole

CAS Number:

65277-42-1

Indication:

For the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.

Mode of Action:

Ketoconazole interacts with 14-_ demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability. Other mechanisms may involve the inhibition of endogenous respiration, interaction with membrane phospholipids, inhibition of yeast transformation to mycelial forms, inhibition of purine uptake, and impairment of triglyceride and/or phospholipid biosynthesis. Ketoconazole can also inhibit the synthesis of thromboxane and sterols such as aldosterone, cortisol, and testosterone.

Pharmacodynamics:

Ketoconazole, like clotrimazole, fluconazole, itraconazole, and miconazole, is an imidazole antifungal agent.

Metabolism:

Hepatic

Toxicity:

Hepatotoxicity, LD₅₀=86 mg/kg (orally in rat)

IUPAC:

1-[4-(4-{[2-(2, 4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1, 3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one

ATC:

D01AC08 G01AF11 J02AB02

PubChem:

47576

DrugBank:

DB01026 (APRD00401)

Formula:

C₉H₇Cl₂N₅

Molecular Mass:

531.431

Synonyms:

2% Ketocanazole Ketoconazol Ketoconazol [INN-Spanish] Ketoconazole [Usan:Ban:Inn:Jan] Ketoconazolum [INN-Latin]

SMILES:

CC(=O)N1CCN(CC1)C1=CC=C(OCC2COC(CN3C=CN=C3)(O2)C2=CC=C(Cl)C=C2Cl)C=C1

AHFS Code:

08:14.08 84:04.08.08

InChi:

XMAYWYJOQHXEEK-UHFFFAOYSA-N

General Reference:

Goeders NE, Peltier RL, Guerin GF: Ketoconazole reduces low dose cocaine self-administration in rats. Drug Alcohol Depend. 1998 Dec 1;53(1):67-77. Pubmed
Berwaerts J, Verhelst J, Mahler C, Abs R: Cushingês syndrome in pregnancy treated by ketoconazole: case report and review of the literature. Gynecol Endocrinol. 1999 Jun;13(3):175-82. Pubmed
Kazy Z, Puho E, Czeizel AE: Population-based case-control study of oral ketoconazole treatment for birth outcomes. Congenit Anom (Kyoto). 2005 Mar;45(1):5-8. Pubmed
Pierard-Franchimont C, Goffin V, Decroix J, Pierard GE: A multicenter randomized trial of ketoconazole 2% and zinc pyrithione 1% shampoos in severe dandruff and seborrheic dermatitis. Skin Pharmacol Appl Skin Physiol. 2002 Nov-Dec;15(6):434-41. Pubmed

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

LGM currently offers Monoclonal Antibodies (mAbs) for non-GMP/R&D use. Please inquire about Monoclonal Antibodies produced under GMP conditions.

Questions? Call our customer API support number 1-(800)-881-8210.

Ask us about this product

API’s From Quality Manufacturers:

Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
Premium quality GMP certified and fully accredited API manufacturing plants
Technical packages as well as access to filed DMF, ASMF or CEP (subject to availability)
Regulatory and technical assistance towards any submission type based on specific customer requirements

Ketoconazole

65277-42-1

Ask us about this product

API’s From Quality Manufacturers:

Find an API Product