Overview
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.
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
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2024/08/19 | Not Applicable | Recruiting | |||
2024/03/12 | Phase 1 | Completed | |||
2022/12/06 | Phase 2 | Recruiting | Hospital Universitario Dr. Jose E. Gonzalez | ||
2021/05/03 | Early Phase 1 | Terminated | |||
2019/12/26 | Phase 1 | Completed | |||
2019/07/30 | Early Phase 1 | Active, not recruiting | |||
2019/02/19 | Phase 3 | UNKNOWN | |||
2019/01/31 | Phase 3 | Completed | |||
2019/01/08 | Early Phase 1 | Terminated | |||
2018/12/04 | Early Phase 1 | Not yet recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| NuCare Pharmaceuticals,Inc. | 66267-400 | ORAL | 200 mg in 1 1 | 3/17/2022 | |
| Bryant Ranch Prepack | 63629-8677 | TOPICAL | 2 g in 100 g | 11/1/2018 | |
| Padagis Israel Pharmaceuticals Ltd | 45802-465 | TOPICAL | 20 mg in 1 mL | 2/21/2017 | |
| RPK Pharmaceuticals, Inc. | 53002-1381 | TOPICAL | 20 mg in 1 mL | 2/21/2017 | |
| Sincerus Florida, LLC | 72934-2112 | TOPICAL | 2 g in 100 g | 5/16/2019 | |
| JEFFERS | 86010-300 | AURICULAR (OTIC) | 2 g in 1000 g | 4/1/2025 | |
| Click Industries LLC | 86173-811 | TOPICAL | 1 g in 100 mL | 3/12/2025 | |
| NORTHSTAR RX LLC | 16714-955 | TOPICAL | 20 mg in 1 g | 5/13/2019 | |
| NuCare Pharmaceuticals,Inc. | 68071-2902 | ORAL | 200 mg in 1 1 | 12/13/2022 | |
| Direct_Rx | 72189-422 | TOPICAL | 20 mg in 1 g | 2/7/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 11/18/2014 | ||
Authorised | 11/18/2014 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| NIZORAL SHAMPOO 20 mg/g | SIN04926P | SHAMPOO | 20 mg/g | 7/10/1990 | |
| YUCOMY SHAMPOO 2% W/W | SIN15990P | SHAMPOO | 20mg/g | 8/17/2020 | |
| SUNAZOL CREAM 2% w/w | SIN09929P | CREAM | 2% w/w | 8/5/1998 | |
| ANTANAZOL CREAM 2% | SIN07997P | CREAM | 2% | 2/4/1995 | |
| DEZOR SHAMPOO 2 % w/v | SIN11580P | SHAMPOO | 2.00 % w/v | 7/7/2001 | |
| FORMYCO TOPICAL CREAM 20 mg/g | SIN11020P | CREAM | 20 mg/g | 7/13/1999 | |
| NITOZOL CREAM 2% | SIN10369P | CREAM | 2% | 11/3/1998 | |
| KETOCONAZOLE TABLETS 200 mg | SIN10955P | TABLET | 200MG | 5/31/1999 | |
| KEZORAL TABLET 200 mg | SIN12152P | TABLET | 200 mg | 12/23/2002 | |
| YUCOMY CREAM 20MG/G | SIN15770P | CREAM | 20mg/g | 8/7/2019 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Ketoconazole Lotion | 国药准字H20040261 | 化学药品 | 洗剂 | 5/28/2020 | |
| Ketoconazole Lotion | 国药准字H20000588 | 化学药品 | 洗剂 | 5/28/2020 | |
| Ketoconazole Lotion | 国药准字H20000700 | 化学药品 | 洗剂 | 7/14/2020 | |
| Ketoconazole Cream | 国药准字H20067249 | 化学药品 | 乳膏剂 | 12/17/2021 | |
| Ketoconazole Cream | 国药准字H20066001 | 化学药品 | 乳膏剂 | 7/15/2020 | |
| Ketoconazole Cream | 国药准字H20023045 | 化学药品 | 软膏剂 | 9/28/2020 | |
| Ketoconazole Cream | 国药准字H20058393 | 化学药品 | 乳膏剂 | 3/25/2020 | |
| Ketoconazole Cream | 国药准字H20074170 | 化学药品 | 乳膏剂 | 8/9/2022 | |
| Ketoconazole Cream | 国药准字H10920111 | 化学药品 | 乳膏剂 | 6/22/2020 | |
| Ketoconazole Cream | 国药准字H52020915 | 化学药品 | 乳膏剂 | 2/21/2020 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| NIZOKOMP CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/21/2003 |
| MCKAY CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/26/2003 |
| GAMMACIN CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/21/2003 |
| DEZOR SHAMPOO 2% | N/A | taisho pharmaceutical (hk) ltd | N/A | N/A | 11/23/2000 |
| KETASOMYCIN CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/21/2003 |
| MEGACIN CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/21/2003 |
| KETOCOMP CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/21/2003 |
| ZINEROL CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/21/2003 |
| FUZO CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/21/2003 |
| BIGODERM CREAM | N/A | unicorn laboratories o/b american unicorn laboratories limited | N/A | N/A | 3/26/2003 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| DAKTAGOLD KETOCONAZOLE 20mg/g cream tube | 71115 | Medicine | A | 9/20/1999 | |
| SEBIZOLE ketoconazole 20 mg/g application bottle | 66821 | Medicine | A | 11/18/1998 | |
| NIZORAL 1% ANTI-DANDRUFF TREATMENT ketoconazole 10 mg/g application bottle (reformulation) | 389572 | Medicine | A | 6/3/2022 | |
| NIZORAL 2% CREAM ketoconazole 20mg/g tube | 13311 | Medicine | A | 8/28/1991 | |
| NIZORAL 1% ANTI-DANDRUFF TREATMENT ketoconazole 10 mg/g application bottle (reformulation) | 339871 | Medicine | A | 7/21/2020 | |
| NIZORAL 2% ANTI-DANDRUFF TREATMENT ketoconazole 20mg/g application bottle | 47013 | Medicine | A | 2/10/1994 |