Ketoconazole

Generic Name: Ketoconazole

Brand Names: Extina, Ketodan, Ketoderm, Nizoral, Xolegel, Ketoconazole HRA

Drug Type: Small Molecule

Chemical Formula: C_₂₆H_₂₈Cl_₂N_₄O_₄

CAS Number: 65277-42-1

Unique Ingredient Identifier: R9400W927I

Background: Ketoconazole is an imidazole antifungal agent used in the prevention and treatment of a variety of fungal infections. It functions by preventing the synthesis of ergosterol, the fungal equivalent of cholesterol, thereby increasing membrane fluidity and preventing growth of the fungus. Ketoconazole was first approved in an oral formulation for systemic use by the FDA in 1981. At this time it was considered a significant improvement over previous antifungals, miconazole and clotrimazole, due to its broad spectrum and good absorption. However, it was discovered that ketoconazole produces frequent gastrointestinal side effects and dose-related hepatitis. These effects combined with waning efficacy led to its eventual replacement by triazole agents, fluconazole, itraconazole, voriconazole, and posaconazole. Ketoconazole and its predecessor clotrimazole continue to be used in topical formulations.

Indication: Ketoconazole is used in the treatment or prevention of fungal infections including blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis. In Europe, it is also used in the treatment of endogenous Cushing's syndrome.

Associated Conditions: Bacterial Vaginosis (BV), Blastomycosis, Candidiasis, Systemic, Chromoblastomycosis, Chronic Mucocutaneous Candidiasis (CMC), Coccidioidomycosis, Dandruff, Endogenous Cushing's Syndrome, Fungal Infections, Histoplasmosis, Paracoccidioidomycosis, Seborrheic Dermatitis, Tinea Corporis caused by Epidermophyton floccosumin, Tinea Corporis caused by Trichophyton mentagrophytes, Tinea Corporis caused by Trichophyton rubrum, Tinea Cruris caused by Epidermophyton floccosumin, Tinea Cruris caused by Trichophyton mentagrophytes, Tinea Cruris caused by Trichophyton rubrum, Tinea Pedis caused by Epidermophyton floccosumin, Tinea Pedis caused by Trichophyton mentagrophytes, Tinea Pedis caused by Trichophyton rubrum, Vaginal Candidiasis, Vulvovaginal Candidiasis, Cutaneous candidiasis, Recalcitrant Dermatophytosis, Tinea versicolor caused by Malassezia infection

Associated Therapies: -

Clinical Trials

A Study to Evaluate the Relative Bioavailability, Food Effect and Effect of Ketoconazole on the Rate and Extent of Absorption of Solid Dosage Formulation(s) of JNJ-40411813

Phase 1

Completed

Conditions: Healthy

Interventions: Drug: Ketoconazole

First Posted Date: 2013-08-30

Last Posted Date: 2013-09-09

Lead Sponsor: Johnson & Johnson Pharmaceutical Research & Development, L.L.C.

Target Recruit Count: 36

Registration Number: NCT01932320

Effect of Ketoconazole on the Pharmacokinetics of Refametinib

Phase 1

Completed

Conditions: Drug Interactions

Interventions: Drug: BAY86-9766
Drug: Ketoconazole

First Posted Date: 2013-08-20

Last Posted Date: 2014-01-08

Lead Sponsor: Bayer

Target Recruit Count: 18

Registration Number: NCT01925638

A Study of Baricitinib When Administered With Ketoconazole or Fluconazole in Healthy Participants

Phase 1

Completed

Conditions: Healthy Volunteers

Interventions: Drug: Baricitinib
Drug: Ketoconazole
Drug: Fluconazole

First Posted Date: 2013-08-16

Last Posted Date: 2017-06-06

Lead Sponsor: Eli Lilly and Company

Target Recruit Count: 36

Registration Number: NCT01924299

Locations: 🇬🇧
For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Leeds, West Yorkshire, United Kingdom

CC-223 and Ketoconazole Drug-Drug Interaction Study

Phase 1

Completed

Conditions: Healthy Volunteers

Interventions: Drug: CC-223
Drug: Ketoconazole

First Posted Date: 2013-07-11

Last Posted Date: 2019-11-12

Lead Sponsor: Celgene

Target Recruit Count: 14

Registration Number: NCT01896323

The Effect of Gemfibrozil, Ketoconazole and Clarithromycin on the Amount of LY2409021 in the Bloodstream

Phase 1

Completed

Conditions: Healthy Volunteers

Interventions: Drug: LY2409021
Drug: Gemfibrozil
Drug: Ketoconazole
Drug: Clarithromycin

First Posted Date: 2013-04-19

Last Posted Date: 2019-03-08

Lead Sponsor: Eli Lilly and Company

Target Recruit Count: 30

Registration Number: NCT01836198

Locations: 🇺🇸
For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician., Evansville, Indiana, United States