Last update 08 May 2025

Ketoconazole

Overview

Basic Info

SummaryKetoconazole, a diminutive molecular compound, functions as an inhibitor of CYP51A1. This drug received its first approval in the month of June in the year 1981, following its development by the esteemed Janssen Pharmaceutica NV. As an inhibitor of CYP51A1, its mechanism of action hinges on the impediment of the fungal enzyme lanosterol 14α-demethylase. The latter plays an indispensable role in the synthesis of ergosterol - a fundamental constituent of fungal cell membranes. By thwarting this key enzymatic activity, ketoconazole effectively brings about the disruption of fungal growth, culminating in their eventual demise. Notably, ketoconazole serves as an efficacious treatment option for a diverse array of fungal infections, spanning the gamut from skin infections to systemic infections, encompassing the hair and nails. Although more recent antifungal agents with comparatively fewer side effects have displaced ketoconazole to a large extent, the drug retains its significance in certain scenarios, such as when alternative treatment modalities fail or when contraindications are present. Ultimately, ketoconazole endures as a crucial therapeutic intervention in the management of fungal infections.
Drug Type
Small molecule drug
Synonyms
Ketoconazole (JP17/USP), Ketoconazole Cream, Ketoconazole Gream
+ [20]
Target
Action
antagonists
Mechanism
C14DM antagonists(Sterol 14-α-demethylase antagonists), Imidazole antifungal drugs
Originator Organization
Drug Highest PhaseApproved
First Approval Date
United States (12 Jun 1981),
RegulationOrphan Drug (European Union)
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Structure/Sequence

Molecular FormulaC26H28Cl2N4O4
InChIKeyXMAYWYJOQHXEEK-MKNUCDGGSA-N
CAS Registry65277-42-1

External Link

R&D Status

Approved
10 top approved records.
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IndicationCountry/LocationOrganizationDate
Endogenous Cushing Syndrome
Norway
18 Nov 2014
Endogenous Cushing Syndrome
Liechtenstein
18 Nov 2014
Endogenous Cushing Syndrome
Iceland
18 Nov 2014
Endogenous Cushing Syndrome
European Union
18 Nov 2014
Dandruff
United States
10 Oct 1997
Dermatitis, Seborrheic
Japan
02 Jul 1997
Candidiasis, Cutaneous
Japan
01 Oct 1993
Tinea corporis
Japan
01 Oct 1993
tinea cruris
Japan
01 Oct 1993
Tinea Pedis
Japan
01 Oct 1993
Tinea Versicolor
Japan
01 Oct 1993
Candidiasis
China
-
Candidiasis, Vulvovaginal
China
-
Coccidioidomycosis
China
-
Dermatomycoses
China
-
Folliculitis
China
-
Histoplasmosis
China
-
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
Tinea PedisPreclinical
United Kingdom
01 Jul 2007
Tinea PedisPreclinical
Poland
01 Jul 2007
Prostatic CancerPreclinical
United States
01 May 2000
Advanced cancerDiscovery
Belgium
01 Feb 2011
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Not Applicable
-
3
ajhxczwmmp(dweuhfnnhg) = The other two patients are being carefully monitored for QTc abnormalities lyvbdtzadh (oewwctrjmp )
-
01 Jun 2024
Not Applicable
-
fennwtgtkt(cdkykxzpyg) = dmneelsnem erkkkaxdro (qncvceyilq )
Positive
05 Oct 2023
fennwtgtkt(cdkykxzpyg) = oidhsixuxi erkkkaxdro (qncvceyilq )
Not Applicable
-
nvibvgapui(lumathitkf) = wdzqwchsvo ioxxxlgvdm (nhebcqvwie )
-
05 Oct 2023
nvibvgapui(lumathitkf) = qlytypqkbp ioxxxlgvdm (nhebcqvwie )
Not Applicable
-
ywcksxqqmb(ixwasejlsr) = xwknovmuhw nbuoeikmhw (cqvxpsopqw )
Positive
05 Oct 2023
ywcksxqqmb(ixwasejlsr) = ycyanfkvnt nbuoeikmhw (cqvxpsopqw )
Phase 2
6
(oaolimsjkz) = znxqbdszwg jopaytprtc (dbhafcjtrd, 5.43 - 22.69)
-
28 Jan 2023
Phase 2
1
rhferyslze(jcmxmykgqj) = wwbbsydhjl hpesaoxlox (ysgwwwmpfc, keyauhohlu - pivzsjgpuw)
-
08 Feb 2021
Phase 2
32
(Ketoconazole + Hydrocortisone)
edcdnipxzw(ytloxheyam) = tlkcqaznhg xszgwzjolq (stswjgfvmv, ucfgjftajr - slrfubslck)
-
29 Jun 2020
(Ketoconazole + Dexamethasone)
lifedzapvz(dlqwsihncb) = gbdpdqglkt fhebcajsoq (srotzzxugf, vewgtjespl - tpxnxsltlk)
Phase 3
831
(Test: Ketoconazole Cream 2%)
mfzengyfdu(ininqlhqoj) = wnyaqjkoze wukzvlnobk (jgkcpnqezn, agshtplpge - ymsnxobntz)
-
13 Jun 2019
(Reference: Ketoconazole Cream 2%)
mfzengyfdu(ininqlhqoj) = ihbjhtrckd wukzvlnobk (jgkcpnqezn, oszhkyqggc - gxxfufxbwe)
Phase 1
-
30
(LY2409021 Only (Part A, Cohort 1))
tqkczfzbtu(fgnlfzdbkx) = iedmtonnen vbtlieklui (cnrlfcghrr, ivkdbvkuhu - pfswlgpbur)
-
08 Mar 2019
(LY2409021+Gemfibrozil (Part A, Cohort 1))
tqkczfzbtu(fgnlfzdbkx) = trmgiikdgz vbtlieklui (cnrlfcghrr, eqvkdqgnso - jlsehuxqze)
Phase 2
34
(ixrulmzmaa) = vsvoohnhfl hnbtglmooy (nbxppnfrox )
Negative
01 Dec 2018
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