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Epinephrine

Other agents for local oral treatment · Local hemostatics · given by inhalation, intramuscular, intravenous, subcutaneous, intramuscular, subcutaneous, · on the market since 1987

5
Leads
30.3M
People
8
Makers
33
How abandoned
01

What it's made of

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

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.

SETS HOW LONG IT LASTS

Phenol

What it does. The liver's favourite attachment point. It tags this group and flushes the molecule out, often within an hour.

What it opens up. Usually shortens the drug's life. Blocking or masking this position is the standard way to make a compound last longer.

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.
Barely
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.
Easily
Urinary tract
Cleared unchanged in urine. Local concentration exceeds plasma.
03

What it binds — and whether we can reach it · 6 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.
ADRA1D
GPCR · agonist
6.66
Just reachable
ADRA2A
GPCR · agonist
6.5600000000000005
Just reachable
ADRA1B
GPCR · agonist
6.5
Just reachable
ADRA2C
GPCR · agonist
6.45
Just reachable
ADRA2B
GPCR · agonist
6.4
Just reachable
ADRB2
GPCR · agonist
6.2
Just reachable
ADRA1A
GPCR · agonist
5.7
Out of reach

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 78 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 — 2

open-angle glaucoma

Animal models only

It reduces disease in animal models; untested in humans.

The condition
Chronic outflow obstruction of the eye's drainage canals that can lead to increased internal eye pressure and optic nerve damage.
ADRB2 · adrenoceptor beta 2
G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, activating bifurcated signaling pathways (PubMed:2831218, PubMed:7915137). ADRB2 binds epinephrine (Epi) with an approximately 30-fold greater affinity than norepinephrine (NE) (PubMed:2831218, PubMed:33093660, PubMed:7915137). In the heart, Epi- and NE-activated ADRB2 induces rapid and slow cardiomyocyte contraction rate, respectively (By similarity). Both NE and Epi promote coupling to G(s)/PKA pathway to regulate myocyte c
Phase 1 only
Safety and dose-finding studies exist. No efficacy data.
NCT04214847 The Outcome of Ahmed Glaucoma Valve in D · NA · 1 people
+1 more on ClinicalTrials.gov
What would kill it. Direction conflict, unless the variant has been assigned the wrong functional class — a known failure mode of consequence-based annotation.

glaucoma

Animal models only

It reduces disease in animal models; untested in humans.

The condition
Increased pressure in the eyeball due to obstruction of the outflow of aqueous humor.
ADRB2 · adrenoceptor beta 2
G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, activating bifurcated signaling pathways (PubMed:2831218, PubMed:7915137). ADRB2 binds epinephrine (Epi) with an approximately 30-fold greater affinity than norepinephrine (NE) (PubMed:2831218, PubMed:33093660, PubMed:7915137). In the heart, Epi- and NE-activated ADRB2 induces rapid and slow cardiomyocyte contraction rate, respectively (By similarity). Both NE and Epi promote coupling to G(s)/PKA pathway to regulate myocyte c
Phase 1 only
Safety and dose-finding studies exist. No efficacy data.
NCT04214847 The Outcome of Ahmed Glaucoma Valve in D · NA · 1 people
+4 more on ClinicalTrials.gov
What would kill it. Direction conflict, unless the variant has been assigned the wrong functional class — a known failure mode of consequence-based annotation.
Already used for these — 3

Established practice, listed so the method can be checked against what is already known.

hypertensive disorder

Already in use

It is already used for this.

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
In routine use
Established practice for this condition, not a new candidate.
NCT07603466 Combination Osilodrostat and Cabergoline · Ph 4 · 50 people
+14 more on ClinicalTrials.gov
What would kill it. Direction conflict, unless the variant has been assigned the wrong functional class — a known failure mode of consequence-based annotation.

asthma

Already in use

It is already used for this.

The condition
A bronchial disease that is characterized by chronic inflammation and narrowing of the airways, which is caused by a combination of environmental and genetic factors resulting in recurring periods of wheezing (a whistling sound while breathing), chest tightness, shortness of breath, mucus production and coughing. The symptoms appear due to a variety of triggers such as allergens, irritants, respiratory infections, weather changes, exercise, stress, reflux disease, medications, foods and emotional anxiety.
ADRB2 · adrenoceptor beta 2
G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, activating bifurcated signaling pathways (PubMed:2831218, PubMed:7915137). ADRB2 binds epinephrine (Epi) with an approximately 30-fold greater affinity than norepinephrine (NE) (PubMed:2831218, PubMed:33093660, PubMed:7915137). In the heart, Epi- and NE-activated ADRB2 induces rapid and slow cardiomyocyte contraction rate, respectively (By similarity). Both NE and Epi promote coupling to G(s)/PKA pathway to regulate myocyte c
In routine use
Established practice for this condition, not a new candidate.
NCT01241006 Single Oral Dose of Dexamethasone Versus · Ph 4 · 376 people
+14 more on ClinicalTrials.gov
What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach ADRB2 in the relevant tissue at tolerated doses.

chronic obstructive pulmonary disease

Already in use

It is already used for this.

The condition
A chronic and progressive lung disorder characterized by the loss of elasticity of the bronchial tree and the air sacs, destruction of the air sacs wall, thickening of the bronchial wall, and mucous accumulation in the bronchial tree. The pathologic changes result in the disruption of the air flow in the bronchial airways. Signs and symptoms include shortness of breath, wheezing, productive cough, and chest tightness. The two main types of chronic obstructive pulmonary disease are chronic obstructive bronchitis and
ADRB2 · adrenoceptor beta 2
G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, activating bifurcated signaling pathways (PubMed:2831218, PubMed:7915137). ADRB2 binds epinephrine (Epi) with an approximately 30-fold greater affinity than norepinephrine (NE) (PubMed:2831218, PubMed:33093660, PubMed:7915137). In the heart, Epi- and NE-activated ADRB2 induces rapid and slow cardiomyocyte contraction rate, respectively (By similarity). Both NE and Epi promote coupling to G(s)/PKA pathway to regulate myocyte c
In routine use
Established practice for this condition, not a new candidate.
NCT01241006 Single Oral Dose of Dexamethasone Versus · Ph 4 · 376 people
+12 more on ClinicalTrials.gov
What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach ADRB2 in the relevant tissue at tolerated doses.
05

Why nobody will fund it

8 companies make this across 12 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 is33 / 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
oraltopicalmodified-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
$8.74
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
3,070 grants on NIH RePORTER
5U01DK135120-04(NIDDK · National Institute of Diabetes & Digestive & Kidney Diseases)Active
$732K (2026)
Restoring awareness of hypoglycemia in type 1 diabetes
PI: Rickels, Michael R · University Of Pennsylvania, Philadelphia, PA · through 2027-12
5U01DK135131-04(NIDDK · National Institute of Diabetes & Digestive & Kidney Diseases)Active
$741K (2026)
Advanced Insulin Delivery to Reduce Impaired Awareness of Hypoglycemia in a T1D Cohort (AIDRIAHT1C)
PI: Pratley, Richard E · Adventhealth Orlando, Orlando, FL · through 2027-12
5R01DK135857-03(NIDDK · National Institute of Diabetes & Digestive & Kidney Diseases)Active
$530K (2026)
Orexin glucose-inhibited neurons and hypoglycemia unawareness
PI: Routh, Vanessa H · Rutgers Biomedical And Health Sciences, Newark, NJ · through 2029-02
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.

American Regent IncAmneal Eu LtdDeva Holding Anonim Sirketi
8
Manufacturers
companies with their own approval
12
Approved products
distinct strengths and forms
4
Routes
inhalation, intramuscular, intravenous, subcutaneous, intramuscular, subcutaneous,
1987
Oldest product still sold
approval year of the earliest product still on the market
ALSO SOLD AS
ADRENACLICKADRENALINAUVI-Q

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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