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

Clinical Trials

Calcitriol in Combination With Ketoconazole and Therapeutic Hydrocortisone in Treating Patients With Prostate Cancer

Phase 1

Terminated

Conditions: Stage IV Prostate Cancer
Stage III Prostate Cancer
Prostate Adenocarcinoma
Recurrent Prostate Carcinoma

Interventions: Dietary Supplement: Calcitriol
Drug: Ketoconazole
Other: Laboratory Biomarker Analysis
Other: Pharmacological Study
Drug: Therapeutic Hydrocortisone

First Posted Date: 2007-09-28

Last Posted Date: 2017-06-14

Lead Sponsor: Roswell Park Cancer Institute

Target Recruit Count: 51

Registration Number: NCT00536991

Locations: 🇺🇸
Roswell Park Cancer Institute, Buffalo, New York, United States

A Study of the Effects of Ketoconazole Taken Orally Has on the PK Profiles of a Dose of GSK189075 in Healthy Volunteers

Phase 1

Completed

Conditions: Diabetes Mellitus, Type 2
Type 2 Diabetes Mellitus

First Posted Date: 2007-07-16

Last Posted Date: 2012-06-04

Lead Sponsor: GlaxoSmithKline

Target Recruit Count: 22

Registration Number: NCT00501397

Locations: 🇺🇸
GSK Investigational Site, Columbus, Ohio, United States

Evaluation Of SB-751689 Administered At Supratherapeutic Dose Levels In Healthy Adult Subjects.

Phase 1

Completed

Conditions: Osteoporosis

First Posted Date: 2007-05-03

Last Posted Date: 2008-10-13

Lead Sponsor: GlaxoSmithKline

Target Recruit Count: 15

Registration Number: NCT00468689

Locations: 🇺🇸
GSK Investigational Site, Baltimore, Maryland, United States

A Study to Assess the Safety and Interaction Between Casopitant and Ketoconazole When Taken By Healthy Adults

Phase 1

Completed

Conditions: Nausea and Vomiting, Chemotherapy-Induced

Interventions: Drug: Casopitant 150 mg
Drug: Casopitant 150 mg matching placebo
Drug: Ketoconazole
Drug: Casopitant 50 mg
Drug: Casopitant 50 mg matching placebo

First Posted Date: 2007-04-16

Last Posted Date: 2017-08-03

Lead Sponsor: GlaxoSmithKline

Target Recruit Count: 85

Registration Number: NCT00460707

Locations: 🇺🇸
GSK Investigational Site, Columbus, Ohio, United States

Treating Patients With Prostate Cancer That Did Not Respond to Hormone Therapy

Phase 2

Completed

Conditions: Prostate Cancer

Interventions: Drug: ketoconazole
Drug: lenalidomide
Drug: therapeutic hydrocortisone

First Posted Date: 2007-04-13

Last Posted Date: 2020-07-24

Lead Sponsor: Case Comprehensive Cancer Center

Target Recruit Count: 34

Registration Number: NCT00460031

Locations: 🇺🇸
UHHS Westlake Medical Center, Cleveland, Ohio, United States
🇺🇸
Cleveland Clinic Taussig Cancer Institute, Case Comprehensive Cancer Center, Cleveland, Ohio, United States
🇺🇸
University Hospitals Cleveland Medical Center, Seidman Cancer Center, Case Comprehensive Cancer Center, Cleveland, Ohio, United States

and more 3 locations