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Clotrimazole

Antiinfectives and antiseptics for local oral treatment · Imidazole and triazole derivatives · given by oral, otic, topical, vaginal · on the market since 1993

5
Leads
17.4M
People
11
Makers
40
How abandoned
01

What it's made of

Each functional group on the molecule does a specific, predictable job.

SETS HOW LONG IT LASTS

Aromatic halogen

What it does. Slows liver breakdown and increases membrane crossing. Also fills space in a binding pocket, which often raises potency several-fold.

What it opens up. Better tissue penetration and longer duration, at the cost of higher fat storage.

CARRIES THE MAIN JOB

Imidazole ring

What it does. Slots directly onto the iron atom at the centre of haem-containing enzymes. That includes the fungal enzyme that builds cell membranes — and also the human liver's main drug-processing enzymes, which is why these compounds interfere with so many other medicines.

What it opens up. Any haem enzyme. The same ring that kills fungi also blocks human steroid synthesis, which is how an antifungal ended up used against hormone-driven disease.

02

Where it can get to

Predicted from molecular weight, lipophilicity, polar surface area and hydrogen-bond donor count. A drug can only act where it distributes, so this constrains which conditions are addressable before any biology is considered. derived

Easily
Systemic circulation
Absorbed from the gut and distributed in plasma.
Easily
Central nervous system
Crosses the blood–brain barrier.
No
Intestinal lumen only
Poorly absorbed. Acts locally in the gut with minimal systemic exposure.
Partly
Skin
Crosses the stratum corneum. Viable as a topical.
Barely
Urinary tract
Cleared unchanged in urine. Local concentration exceeds plasma.
03

What it binds — and whether we can reach it · 8 of 7 reachable

Binding affinity is only meaningful against the plasma concentration reached at the approved dose. A target requiring higher concentrations cannot be engaged in a patient, whatever the in vitro potency. Most repurposing hypotheses fail at this step, and it is rarely checked before a trial is proposed. measured

Values are pAct — the negative logarithm of the molar concentration at which the drug half-occupies the target. Each whole step is a tenfold difference in potency: 9.0 = 1 nanomolar, 6.0 = 1 micromolar, 5.0 = 10 micromolar. Oral drugs typically reach 0.1–10 micromolar in plasma, so roughly 6.0 is the threshold below which a target cannot be reached at a tolerated dose. Figures come from DrugCentral’s curated binding data.
CYP19A1
Enzyme ·
8.74
Engaged easily
TBXAS1
Enzyme ·
7.85
Engaged
CYP2C19
Enzyme ·
7.8
Engaged
CYP2C9
Enzyme ·
7.8
Engaged
CYP3A4
Enzyme ·
7.7
Engaged
KCNN4
Ion channel ·
7.15
Engaged
CYP17A1
Enzyme ·
7.09
Engaged
04

New uses, and who is already trying them

One card per candidate indication: the reasoning link by link, the evidence tier that governs how strongly it can be stated, and any registered trials.

5 of the 58 conditions linked to this drug’s targets have been checked against trial records so far. The rest are not ruled out — they are unchecked.

Not yet used for these — 5

congenital adrenal hyperplasia due to 17-alpha-hydro

Wide open

It acts on a target linked to this disease; untested, and the direction of effect is unverified.

The condition
A very rare form of congenital adrenal hyperplasia (CAH) characterized by glucocorticoid deficiency, hypergonadotrophic hypogonadism and severe hypokalemic hypertension.
CYP17A1 · cytochrome P450 family 17 subfamily A member 1
A cytochrome P450 monooxygenase involved in corticoid and androgen biosynthesis (PubMed:22266943, PubMed:25301938, PubMed:27339894, PubMed:9452426). Catalyzes 17-alpha hydroxylation of C21 steroids, which is common for both pathways. A second oxidative step, required only for androgen synthesis, involves an acyl-carbon cleavage. The 17-alpha hydroxy intermediates, as part of adrenal glucocorticoids biosynthesis pathway, are precursors of cortisol (Probable) (PubMed:25301938, PubMed:9452426). Hydroxylates steroid ho
Nobody has tried this
No registered trial of this drug in this condition.
What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach CYP17A1 in the relevant tissue at tolerated doses.

ghosal hematodiaphyseal dysplasia

Wide open

It acts on a target linked to this disease; untested, and the direction of effect is unverified.

The condition
Ghosal hematodiaphyseal dysplasia syndrome (GHDD) is a rare disorder characterized by increased bone density (predominantly diaphyseal) and aregenerative corticosteroid-sensitive anemia.
TBXAS1 · thromboxane A synthase 1
Catalyzes the conversion of prostaglandin H2 (PGH2) to thromboxane A2 (TXA2), a potent inducer of blood vessel constriction and platelet aggregation (PubMed:11097184, PubMed:11297515, PubMed:22735388, PubMed:24009185, PubMed:8436233, PubMed:9873013). Also cleaves PGH2 to 12-hydroxy-heptadecatrienoicacid (12-HHT) and malondialdehyde, which is known to act as a mediator of DNA damage. 12- HHT and malondialdehyde are formed stoichiometrically in the same amounts as TXA2 (PubMed:11297515, PubMed:22735388, PubMed:987301
Nobody has tried this
No registered trial of this drug in this condition.
What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach TBXAS1 in the relevant tissue at tolerated doses.

aromatase deficiency

Wide open

It acts on a target linked to this disease; untested, and the direction of effect is unverified.

The condition
Aromatase deficiency disrupts the synthesis of estradiol, resulting in hirsutism of mothers during gestation of an affected child; pseudohermaphroditism and virilization in women; and tall stature, osteoporosis and obesity in men.
CYP19A1 · cytochrome P450 family 19 subfamily A member 1
A cytochrome P450 monooxygenase that catalyzes the conversion of C19 androgens, androst-4-ene-3,17-dione (androstenedione) and testosterone to the C18 estrogens, estrone and estradiol, respectively (PubMed:27702664, PubMed:2848247). Catalyzes three successive oxidations of C19 androgens: two conventional oxidations at C19 yielding 19-hydroxy and 19-oxo/19-aldehyde derivatives, followed by a third oxidative aromatization step that involves C1-beta hydrogen abstraction combined with cleavage of the C10-C19 bond to yi
Nobody has tried this
No registered trial of this drug in this condition.
What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach CYP19A1 in the relevant tissue at tolerated doses.

dehydrated hereditary stomatocytosis

Wide open

It acts on a target linked to this disease; untested, and the direction of effect is unverified.

The condition
Dehydrated hereditary stomatocytosis (DHS) is a rare hemolytic anemia characterized by a decreased red cell osmotic fragility due to a defect in cation permeability, resulting in red cell dehydration and mild to moderate compensated hemolysis. Pseudohyperkalemia (loss of potassium ions from red cells on storage at room temperature) is sometimes observed.
KCNN4 · potassium calcium-activated channel subfamily N member 4
Intermediate conductance calcium-activated potassium channel that mediates the voltage-independent transmembrane transfer of potassium across the cell membrane through a constitutive interaction with calmodulin which binds the intracellular calcium allowing its opening (PubMed:10026195, PubMed:10961988, PubMed:11425865, PubMed:15831468, PubMed:17157250, PubMed:18796614, PubMed:26148990, PubMed:9326665, PubMed:9380751, PubMed:9407042). The current is characterized by a voltage-independent activation, an intracellula
Nobody has tried this
No registered trial of this drug in this condition.
What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach KCNN4 in the relevant tissue at tolerated doses.

46,XY disorder of sex development due to isolated 17

Wide open

It acts on a target linked to this disease; untested, and the direction of effect is unverified.

The condition
No description on file.
CYP17A1 · cytochrome P450 family 17 subfamily A member 1
A cytochrome P450 monooxygenase involved in corticoid and androgen biosynthesis (PubMed:22266943, PubMed:25301938, PubMed:27339894, PubMed:9452426). Catalyzes 17-alpha hydroxylation of C21 steroids, which is common for both pathways. A second oxidative step, required only for androgen synthesis, involves an acyl-carbon cleavage. The 17-alpha hydroxy intermediates, as part of adrenal glucocorticoids biosynthesis pathway, are precursors of cortisol (Probable) (PubMed:25301938, PubMed:9452426). Hydroxylates steroid ho
Nobody has tried this
No registered trial of this drug in this condition.
What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach CYP17A1 in the relevant tissue at tolerated doses.
05

Why nobody will fund it

11 companies make this across 13 approved products. With that many manufacturers the price has fallen to production cost. A company funding a trial could not recover it — competitors could market the same molecule for the new indication immediately, without contributing.

How abandoned it is40 / 100
0 to 100, calculated from manufacturer count, remaining patent or exclusivity, and whether any reformulation route to exclusivity is still open. 100 means no route to commercial return exists. The weights behind it are unsourced.
THE ONE WAY A COMPANY COULD STILL OWN IT
injectableinhaledmodified-release

A new route or dosage form qualifies for a 505(b)(2) application, which carries three years of exclusivity for that formulation. It is the only remaining route to exclusivity on a generic molecule.

06

What it would cost to find out

Derived, not quoted. Events needed is 4(zα+zβ)²/ln(HR)²; enrolment is that divided by the event rate and follow-up. The 1/ln(HR)² term dominates: halving the detectable effect size roughly quadruples enrolment. derived

0.75
Lower = bigger effect = smaller trial
8.0%
2 yr
$32K
Unsourced placeholder
379
Events needed
3K
Patients
$93M
Trial cost
assumed
$15.20
Per person reached
assumed

Cost per person reached is the relevant metric for a non-commercial funder, since there is no revenue to set against the outlay.

07

Ask for ideas nobody has listed

Reasons from the functional groups and distribution above, excluding conditions already listed. Output is hypotheses for falsification, not findings. Not medical advice.

08

Who might pay for the trial

Trials of off-patent drugs are rarely funded by venture capital or pharma. They are paid for by government grants and disease foundations. Here is who has funded work on this molecule before, what federal mechanisms are open now, and which foundations fund trials in the disease areas it touches. measured

Federal grants that name this medicine
133 grants on NIH RePORTER
2R01AI155413-06A1(NIAID · National Institute of Allergy & Infectious Diseases)Active
$379K (2026)
Slo-1 and TRP-2 channel interacting drug targets in filaria
PI: Martin, Richard John · Iowa State University, Ames, IA · through 2031-07
1R43AI191888-01(NIAID · National Institute of Allergy & Infectious Diseases)Concluded
$299K (2025)
Novel, bio-inspired chloramine to treat cutaneous fungal infections without resistance generation potential
PI: Hein, Marc D. · Halomine, Inc., Ithaca, NY · through 2026-07
5R01AR073324-05(NIAMS · National Institute of Arthritis & Musculoskeletal Diseases)Concluded
$344K (2022)
Targeting hexokinase-2 in rheumatoid arthritis
PI: Guma, Monica · University Of California, San Diego, La Jolla, CA · through 2024-05
Open federal programmes that would fund this work

Open notices with an explicit mandate to fund work on approved or off-patent molecules.

RFA-CA-25-033National Institutes of HealthForecast — not open yet
Glioblastoma Therapeutics Network (GTN; U19 Clinical Trial Required)
RFA-FD-25-020Food and Drug Administrationcloses 05/16/2028
Reissue of RFA-FD-23-001- Clinical Studies of Orphan Products Addressing Unmet
FOR-FD-25-020Food and Drug AdministrationForecast — not open yet
Clinical Studies of Orphan Products Addressing Unmet Needs of Rare Diseases (R
FOR-FD-25-001Food and Drug AdministrationForecast — not open yet
Clinical Trials Addressing Unmet Needs of Rare Neurodegenerative Diseases (R01
RFA-TR-25-002National Institutes of Healthcloses 07/02/2027
Preclinical Proof of Concept Studies for Rare Diseases (R21 Clinical Trial Not
PAR-25-374National Institutes of Healthcloses 05/07/2028
Translational Bioinformatics and Experimental Approaches to Advance Drug Repos
HT942526PRCRPCTADefense Health Agency Contracting Activity -closes 10/05/2026
DoW Peer Reviewed Cancer, Clinical Trial Award
PAR-26-049National Institutes of HealthForecast — not open yet
Establishing Pediatric CNS Pharmacodynamic Measures as Tools to Enable Psychia
Showing 8 of 990 currently open under this category on Grants.gov, matched to the disease areas this drug touches. derived Browse all 990 on Grants.gov ↗
Funders beyond the federal system

Grants.gov lists US federal money. Many off-patent drug trials are supported by disease foundations and nonprofits. These are matched to the body systems this drug touches. assumed

Matched by disease area, not by molecule — a foundation appearing here funds work in a field this drug touches.
09

Who manufactures it

Companies holding an approved abbreviated application for this molecule in the United States, from the FDA Orange Book. Supply already exists at scale, so a trial would not need a manufacturing programme — but any of these could also be a partner, or an objector.

Encube Ethicals Private LtdFougera Pharmaceuticals IncGlenmark Pharmaceuticals Inc Usa
11
Manufacturers
companies with their own approval
13
Approved products
distinct strengths and forms
4
Routes
oral, otic, topical, vaginal
1993
Oldest product still sold
approval year of the earliest product still on the market
ALSO SOLD AS
CLOTICTRIVAGIZOLE 3

Nothing on this page is medical advice. Candidate uses are unproven hypotheses derived from public data; established uses are listed for verification only. Figures carry their provenance inline — anything marked assumed or derived is not a measurement.

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