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Tamsulosin Hydrochloride

Alpha-adrenoreceptor antagonists · given by oral · on the market since 2010

5
Leads
49.3M
People
11
Makers
55
How abandoned
01

What it's made of

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

GRABS METAL

Primary sulfonamide

What it does. Latches onto zinc atoms held inside enzymes. Humans have at least fifteen zinc enzymes called carbonic anhydrases, and they sit in the eye, the kidney, the stomach lining, bone, and the brain — all doing the same chemistry in different rooms.

What it opens up. Any tissue that runs a carbonic anhydrase is potentially reachable. This is the exact reason a diuretic became a glaucoma drug, an altitude-sickness drug, and a treatment for pressure build-up around the brain — one claw, five rooms.

GRABS METAL

Catechol

What it does. Chemically unstable in the body and destroyed within minutes by a dedicated enzyme. Also chelates iron.

What it opens up. Almost always a liability, not an asset: it caps how long the drug lasts and usually forces a second drug alongside it to block the breakdown.

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.

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.
Partly
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.
Partly
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.
ADRA1A
GPCR ·
10.54
Engaged easily
ADRA1D
GPCR ·
10.24
Engaged easily
DRD3
GPCR ·
9.55
Engaged easily
ADRA1B
GPCR ·
9.21
Engaged easily
HTR1A
GPCR ·
9.1
Engaged easily
ADRA2C
GPCR ·
8.1
Engaged easily
DRD2
GPCR ·
7.89
Engaged

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 102 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

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.
DRD2 · dopamine receptor D2
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528, PubMed:39103320). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity). {ECO:0000250|UniProtKB:P61168, ECO:0000269|PubMed:21645528, ECO:0000269|PubMed:39103320}.
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 DRD2 in the relevant tissue at tolerated doses.

schizophrenia

Wide open

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

The condition
A major psychotic disorder characterized by abnormalities in the perception or expression of reality. It affects the cognitive and psychomotor functions. Common clinical signs and symptoms include delusions, hallucinations, disorganized thinking, and retreat from reality.
DRD2 · dopamine receptor D2
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528, PubMed:39103320). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity). {ECO:0000250|UniProtKB:P61168, ECO:0000269|PubMed:21645528, ECO:0000269|PubMed:39103320}.
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 DRD2 in the relevant tissue at tolerated doses.

bipolar disorder

Wide open

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

The condition
A disorder of the brain that causes unusual shifts in mood, energy, activity levels and the ability to carry out day-to-day tasks. Often these moods range and shift from periods of elation and energized behavior to those of hopelessness and depression.
DRD2 · dopamine receptor D2
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528, PubMed:39103320). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity). {ECO:0000250|UniProtKB:P61168, ECO:0000269|PubMed:21645528, ECO:0000269|PubMed:39103320}.
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 DRD2 in the relevant tissue at tolerated doses.

hypertensive disorder

Animal models only

It reduces disease in animal models; untested in humans.

The condition
Persistently high systemic arterial blood pressure. Based on multiple readings (blood pressure determination), hypertension is currently defined as when systolic pressure is consistently greater than 140 mm Hg or when diastolic pressure is consistently 90 mm Hg or more.
ADRA1D · adrenoceptor alpha 1D
Alpha-1 adrenergic receptors are G protein-coupled receptors for catecholamines that signal through the G(q) family of G proteins, including G(q) and G(11). Upon activation, they stimulate the phosphatidylinositol-calcium second messenger pathway, leading to calcium release from intracellular stores and activation of protein kinase C (PubMed:7746284). ADRA1D binds the catecholamine ligands norepinephrine and epinephrine (PubMed:7815325, PubMed:8024574, PubMed:8183249). {ECO:0000269|PubMed:7746284, ECO:0000269|PubMe
Phase 1 only
Safety and dose-finding studies exist. No efficacy data.
NCT00223717 Treatment of Supine Hypertension in Auto · Ph 1 · 152 people
What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach ADRA1D in the relevant tissue at tolerated doses.

depressive disorder

Wide open

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

The condition
A melancholy feeling of sadness and despair.
DRD2 · dopamine receptor D2
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528, PubMed:39103320). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity). {ECO:0000250|UniProtKB:P61168, ECO:0000269|PubMed:21645528, ECO:0000269|PubMed:39103320}.
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 DRD2 in the relevant tissue at tolerated doses.
05

Why nobody will fund it

11 companies make this across 11 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
$5.38
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
28 grants on NIH RePORTER
5R01DK134386-04(NIDDK · National Institute of Diabetes & Digestive & Kidney Diseases)Active
$699K (2026)
Nitric Oxide-Soluble Guanylate Cyclase Pathway as a Target for Male Bladder Outlet Obstruction and Lower Urinary Tract Symptoms in Aging
PI: Kanai, Anthony John · University Of Pittsburgh At Pittsburgh, Pittsburgh, PA · through 2027-06
1ZIALM010008-10(NLM · National Library of Medicine)Active
$1.2M (2025)
Clinical and Informatics Research on Large Clinical Databases
PI: Mcdonald, Clement · National Library Of Medicine
5R01DK134386-03(NIDDK · National Institute of Diabetes & Digestive & Kidney Diseases)Concluded
$699K (2025)
Nitric Oxide-Soluble Guanylate Cyclase Pathway as a Target for Male Bladder Outlet Obstruction and Lower Urinary Tract Symptoms in Aging
PI: Kanai, Anthony John · University Of Pittsburgh At Pittsburgh, Pittsburgh, PA · through 2027-06
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.

Alkem Laboratories LtdAscent Pharmaceuticals IncAurobindo Pharma Ltd
11
Manufacturers
companies with their own approval
11
Approved products
distinct strengths and forms
1
Routes
oral
2010
Oldest product still sold
approval year of the earliest product still on the market

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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