Ofloxacin

Fluoroquinolones · Antiinfectives · given by ophthalmic, oral, otic · on the market since 1993

5
Leads
47.9M
People
14
Makers
55
How abandoned
01

What it's made of

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

SETS WHERE IT GOES

Carboxylic acid

What it does. At the pH of blood this group is ionised, which means the molecule is permanently charged. Charged molecules stick tightly to blood proteins, get filtered by the kidney, and are largely locked out of the brain.

What it opens up. Excellent for anything in the bloodstream, joints, or kidney. Effectively rules out brain targets unless a transporter carries it in.

SETS WHERE IT GOES

Basic amine

What it does. Neutral enough to slip through membranes, then becomes charged inside the acidic compartments of the cell and gets trapped there. Concentrations inside cells can reach many times the blood level.

What it opens up. Diseases of the cell's internal recycling compartments, and a common reason a drug accumulates in lung, liver, and eye tissue far beyond what the blood level suggests.

SETS HOW LONG IT LASTS

Aromatic fluorine

What it does. The liver attacks rings at predictable positions. Fluorine is small enough not to disturb the shape but strong enough that the attack fails, so the molecule survives longer.

What it opens up. Mainly a durability upgrade, but it also nudges the molecule into being slightly greasier, which helps it enter the brain.

CARRIES THE MAIN JOB

Quinolone core

What it does. Traps the enzyme that unwinds DNA mid-cut, converting a repair machine into a source of DNA breaks.

What it opens up. Bacterial by design, but the human equivalent enzyme is a known cancer target, so the frame recurs in oncology.

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.
Easily
Skin
Crosses the stratum corneum. Viable as a topical.
Easily
Urinary tract
Cleared unchanged in urine. Local concentration exceeds plasma.
03

What it binds — and whether we can reach it

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.
HRH3
GPCR ·
4.55
Not reachable
SLC6A4
Transporter ·
4.54
Not reachable
CHRM1
GPCR ·
4.41
Not reachable
GABRA2
Ion channel ·
4.23
Not reachable

This molecule builds up inside cells far above blood levels, concentrates in urine. Local concentration therefore exceeds plasma, so targets that look unreachable on a plasma reading may still be engaged. assumed

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 99 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

alcohol dependence

Wide open

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

The condition
Physical and psychological dependence on alcohol.
GABRA2 · gamma-aminobutyric acid type A receptor subunit alpha2
Alpha subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain (PubMed:10449790, PubMed:29961870, PubMed:31032849). GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interfaces (By similarity). When activated by GABA, GABAARs selectively allow the flow of chloride anions
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 GABRA2 in the relevant tissue at tolerated doses.

obsessive-compulsive disorder

Wide open

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

The condition
A disorder characterized by the presence of persistent and recurrent irrational thoughts (obsessions), resulting in marked anxiety and repetitive excessive behaviors (compulsions) as a way to try to decrease that anxiety.
SLC6A4 · solute carrier family 6 member 4
Serotonin transporter that cotransports serotonin with one Na(+) ion in exchange for one K(+) ion and possibly one proton in an overall electroneutral transport cycle. Transports serotonin across the plasma membrane from the extracellular compartment to the cytosol thus limiting serotonin intercellular signaling (PubMed:10407194, PubMed:12869649, PubMed:21730057, PubMed:27049939, PubMed:27756841, PubMed:34851672). Essential for serotonin homeostasis in the central nervous system. In the developing somatosensory cor
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 SLC6A4 in the relevant tissue at tolerated doses.

Parkinson disease

Wide open

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

The condition
A progressive degenerative disorder of the central nervous system characterized by loss of dopamine producing neurons in the substantia nigra and the presence of Lewy bodies in the substantia nigra and locus coeruleus. Signs and symptoms include tremor which is most pronounced during rest, muscle rigidity, slowing of the voluntary movements, a tendency to fall back, and a mask-like facial expression.
CHRM1 · cholinergic receptor muscarinic 1
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
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 CHRM1 in the relevant tissue at tolerated doses.

genetic developmental and epileptic encephalopathy

Wide open

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

The condition
A complex neurodevelopmental disorder characterized by a range of developmental delays and epileptic encephalopathy phenotypes. Seizure onset is variable and intellectual disability is variable in presence and severity.
GABRA2 · gamma-aminobutyric acid type A receptor subunit alpha2
Alpha subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain (PubMed:10449790, PubMed:29961870, PubMed:31032849). GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interfaces (By similarity). When activated by GABA, GABAARs selectively allow the flow of chloride anions
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 GABRA2 in the relevant tissue at tolerated doses.

major depressive disorder

Wide open

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

The condition
An episode of depression lasting two or more weeks without an intervening episode of mania.
SLC6A4 · solute carrier family 6 member 4
Serotonin transporter that cotransports serotonin with one Na(+) ion in exchange for one K(+) ion and possibly one proton in an overall electroneutral transport cycle. Transports serotonin across the plasma membrane from the extracellular compartment to the cytosol thus limiting serotonin intercellular signaling (PubMed:10407194, PubMed:12869649, PubMed:21730057, PubMed:27049939, PubMed:27756841, PubMed:34851672). Essential for serotonin homeostasis in the central nervous system. In the developing somatosensory cor
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 SLC6A4 in the relevant tissue at tolerated doses.
05

Why nobody will fund it

14 companies make this across 26 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 is55 / 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
topicalinjectableinhaledmodified-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
$5.54
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
53 grants on NIH RePORTER
1R41DC020077-01(NIDCD · NIDCD)Concluded
$257K (2021)
Synthetic Antimicrobial Peptoids for Treatment of Chronic Suppurative Otitis Media
PI: Kirshenbaum, Kent W · Maxwell Biosciences, Inc., Austin, TX · through 2023-08
1R41EY032437-01(NEI · National Eye Institute)Concluded
$257K (2021)
Novel Ophthalmic Product for Corneal Infections and Injuries
PI: Pereira, Heloise Anne · Biolytx Pharmaceuticals Corp, Oklahoma City, OK · through 2023-09
5R21AI154097-02(NIAID · National Institute of Allergy & Infectious Diseases)Concluded
$198K (2021)
Development of Nanoparticle Antibiotic Adjuvant for the Treatment of Chronic Suppurative Otitis Media
PI: Santa Maria, Peter Luke · Stanford University, Stanford, CA · through 2022-06
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.

Altaire Pharmaceuticals IncAmneal Eu LtdApotex Inc
14
Manufacturers
companies with their own approval
26
Approved products
distinct strengths and forms
3
Routes
ophthalmic, oral, otic
1993
Oldest product still sold
approval year of the earliest product still on the market
ALSO SOLD AS
OCUFLOX

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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