Erlotinib Hydrochloride

Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors · given by oral · on the market since 2014

Leads

23.4M

People

Makers

How abandoned

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.

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.

Intestinal lumen only

Poorly absorbed. Acts locally in the gut with minimal systemic exposure.

Easily

Skin

Crosses the stratum corneum. Viable as a topical.

Partly

Urinary tract

Cleared unchanged in urine. Local concentration exceeds plasma.

What it binds — and whether we can reach it · 1 of 1 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.

EGFR

Kinase · inhibitor

9.22

Engaged easily

Target	Kind	Action	Affinity (pAct)	Can it be engaged?
EGFR	Kinase	inhibitor	9.22	Engaged easily

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 57 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 — 4

non-small cell lung carcinoma

Tried in people

It showed an effect in a human trial that was not followed up.

The condition

A group of at least three distinct histological types of lung cancer, including non-small cell squamous cell carcinoma, adenocarcinoma, and large cell carcinoma. Non-small cell lung carcinomas have a poor response to conventional chemotherapy.

EGFR · epidermal growth factor receptor

Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses (PubMed:10805725, PubMed:27153536, PubMed:2790960, PubMed:35538033). Known ligands include EGF, TGFA/TGF- alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF (PubMed:12297049, PubMed:15611079, PubMed:17909029, PubMed:20837704, PubMed:27153536, PubMed:2790960, PubMed:7679104, PubMed:8144591, PubMed:9419975). Ligand

Open Targets scores each kind of evidence from 0.00 to 1.00 for this exact pairing — EGFR and non-small cell lung carcinoma. The score reflects how much evidence of that kind exists and how consistent it is. It is not a probability that the drug works. Rows are ordered by how much each kind counts toward the evidence figure used in the ranking, not by its raw score, because the two disagree: literature co-occurrence saturates near 1.00 on almost any well-studied pair, while genetic association rarely exceeds 0.70 even when causal.

Genetic association0.75 / 1.00

Inherited variants in this gene alter disease risk in human populations. The datatype most predictive of later clinical success.55% of evidence score

Somatic mutation0.83 / 1.00

This gene is recurrently mutated in this tumour type.15% of evidence score

Pathway0.82 / 1.00

The gene sits in a pathway with established disruption in this condition.8% of evidence score

Curated genetic literature0.61 / 1.00

Gene–disease links curated from published genetic studies.5% of evidence score

Literature co-occurrence1.00 / 1.00

Gene and condition appear together in published text. Reflects publication volume, not causal evidence.2% of evidence score

Clinical1.00 / 1.00

Derived from clinical or trial records.not counted

Phase 3 has run

A Phase 3 trial exists. Read its result before anything else.

NCT00275132 Erlotinib in Treating Patients With Stag · Ph 3 · 670 people

+14 more on ClinicalTrials.gov

What would kill it. A null result in the completed Phase 3.

cancer

Tried in people

It showed an effect in a human trial that was not followed up.

The condition

A tumor composed of atypical neoplastic, often pleomorphic cells that invade other tissues. Malignant neoplasms often metastasize to distant anatomic sites and may recur after excision. The most common malignant neoplasms are carcinomas (adenocarcinomas or squamous cell carcinomas), Hodgkin and non-Hodgkin lymphomas, leukemias, melanomas, and sarcomas.

EGFR · epidermal growth factor receptor

Open Targets scores each kind of evidence from 0.00 to 1.00 for this exact pairing — EGFR and cancer. The score reflects how much evidence of that kind exists and how consistent it is. It is not a probability that the drug works. Rows are ordered by how much each kind counts toward the evidence figure used in the ranking, not by its raw score, because the two disagree: literature co-occurrence saturates near 1.00 on almost any well-studied pair, while genetic association rarely exceeds 0.70 even when causal.

Pathway0.99 / 1.00

The gene sits in a pathway with established disruption in this condition.8% of evidence score

Literature co-occurrence0.99 / 1.00

Gene and condition appear together in published text. Reflects publication volume, not causal evidence.2% of evidence score

Clinical0.79 / 1.00

Derived from clinical or trial records.not counted

Phase 3 has run

A Phase 3 trial exists. Read its result before anything else.

NCT00442455 Erlotinib,Radiation and Cisplatin in Pat · Ph 3 · 53 people

+14 more on ClinicalTrials.gov

What would kill it. A null result in the completed Phase 3.

head and neck squamous cell carcinoma

Tried in people

It showed an effect in a human trial that was not followed up.

The condition

A squamous cell carcinoma that arises from any of the following anatomic sites: lip and oral cavity, nasal cavity, paranasal sinuses, pharynx, larynx, and salivary glands.

EGFR · epidermal growth factor receptor

Open Targets scores each kind of evidence from 0.00 to 1.00 for this exact pairing — EGFR and head and neck squamous cell carcinoma. The score reflects how much evidence of that kind exists and how consistent it is. It is not a probability that the drug works. Rows are ordered by how much each kind counts toward the evidence figure used in the ranking, not by its raw score, because the two disagree: literature co-occurrence saturates near 1.00 on almost any well-studied pair, while genetic association rarely exceeds 0.70 even when causal.

Genetic association0.82 / 1.00

Inherited variants in this gene alter disease risk in human populations. The datatype most predictive of later clinical success.55% of evidence score

Somatic mutation0.46 / 1.00

This gene is recurrently mutated in this tumour type.15% of evidence score

Pathway0.61 / 1.00

The gene sits in a pathway with established disruption in this condition.8% of evidence score

Literature co-occurrence0.99 / 1.00

Gene and condition appear together in published text. Reflects publication volume, not causal evidence.2% of evidence score

Clinical0.88 / 1.00

Derived from clinical or trial records.not counted

Phase 3 has run

A Phase 3 trial exists. Read its result before anything else.

NCT00442455 Erlotinib,Radiation and Cisplatin in Pat · Ph 3 · 53 people

+14 more on ClinicalTrials.gov

What would kill it. A null result in the completed Phase 3.

lung cancer

Tried in people

It showed an effect in a human trial that was not followed up.

The condition

A malignant neoplasm involving the lung.

EGFR · epidermal growth factor receptor

Open Targets scores each kind of evidence from 0.00 to 1.00 for this exact pairing — EGFR and lung cancer. The score reflects how much evidence of that kind exists and how consistent it is. It is not a probability that the drug works. Rows are ordered by how much each kind counts toward the evidence figure used in the ranking, not by its raw score, because the two disagree: literature co-occurrence saturates near 1.00 on almost any well-studied pair, while genetic association rarely exceeds 0.70 even when causal.

Genetic association0.79 / 1.00

Inherited variants in this gene alter disease risk in human populations. The datatype most predictive of later clinical success.55% of evidence score

Somatic mutation0.70 / 1.00

This gene is recurrently mutated in this tumour type.15% of evidence score

Curated genetic literature0.61 / 1.00

Gene–disease links curated from published genetic studies.5% of evidence score

Literature co-occurrence1.00 / 1.00

Gene and condition appear together in published text. Reflects publication volume, not causal evidence.2% of evidence score

Clinical0.84 / 1.00

Derived from clinical or trial records.not counted

Phase 3 has run

A Phase 3 trial exists. Read its result before anything else.

NCT00275132 Erlotinib in Treating Patients With Stag · Ph 3 · 670 people

+14 more on ClinicalTrials.gov

What would kill it. A null result in the completed Phase 3.

Already used for these — 1

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

lung adenocarcinoma

Already in use

It is already used for this.

The condition

A carcinoma that arises from the lung and is characterized by the presence of malignant glandular epithelial cells. There is a male predilection with a male to female ratio of 2:1. Usually lung adenocarcinoma is asymptomatic and is identified through screening studies or as an incidental radiologic finding. If clinical symptoms are present they include shortness of breath, cough, hemoptysis, chest pain, and fever. Tobacco smoke is a known risk factor.

EGFR · epidermal growth factor receptor

Open Targets scores each kind of evidence from 0.00 to 1.00 for this exact pairing — EGFR and lung adenocarcinoma. The score reflects how much evidence of that kind exists and how consistent it is. It is not a probability that the drug works. Rows are ordered by how much each kind counts toward the evidence figure used in the ranking, not by its raw score, because the two disagree: literature co-occurrence saturates near 1.00 on almost any well-studied pair, while genetic association rarely exceeds 0.70 even when causal.

Genetic association0.72 / 1.00

Inherited variants in this gene alter disease risk in human populations. The datatype most predictive of later clinical success.55% of evidence score

Somatic mutation0.87 / 1.00

This gene is recurrently mutated in this tumour type.15% of evidence score

Pathway0.83 / 1.00

The gene sits in a pathway with established disruption in this condition.8% of evidence score

Literature co-occurrence0.99 / 1.00

Gene and condition appear together in published text. Reflects publication volume, not causal evidence.2% of evidence score

Clinical0.66 / 1.00

Derived from clinical or trial records.not counted

In routine use

Established practice for this condition, not a new candidate.

NCT02399566 Clinical Trial of Erlotinib and Pemetrex · Ph 4 · 300 people

+14 more on ClinicalTrials.gov

What would kill it. A null trial, or pharmacokinetic data showing the drug does not reach EGFR in the relevant tissue at tolerated doses.

Why nobody will fund it

8 companies make this across 23 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 is48 / 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.

What it would cost to find out

Derived, not quoted. Events needed is 4(z_α+z_β)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

Effect sought (hazard ratio)0.75

Lower = bigger effect = smaller trial

How often the event happens per year8.0%

Follow-up2 yr

Cost per patient$32K

Unsourced placeholder

379

Events needed

Patients

$93M

Trial cost

assumed

$11.34

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.

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.

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

814 grants on NIH RePORTER

5R01DK132781-04(NIDDK · National Institute of Diabetes & Digestive & Kidney Diseases)Active

$482K (2026)

Primary cilia loss in bile duct cells- the interplay with the autophagy machinery

PI: Gradilone, Sergio A · University Of Minnesota, Minneapolis, MN · through 2027-01

View on NIH RePORTER ↗Apply to same mechanism (PA-20-185) ↗

1R03OD039968-01(OD · OD)Active

$120K (2026)

Establishing pre-clinical models of osimertinib resistance-mediated brain metastasis

PI: Wettersten, Hiromi Inoue · University Of California, San Diego, La Jolla, CA · through 2028-06

View on NIH RePORTER ↗Apply to same mechanism (PAR-25-176) ↗

5R01DK121789-07(NIDDK · National Institute of Diabetes & Digestive & Kidney Diseases)Active

$706K (2026)

Molecular Magnetic Resonance of Hepatic Fibrogenesis

PI: Caravan, Peter D · Massachusetts General Hospital, Boston, MA · through 2028-03

View on NIH RePORTER ↗Apply to same mechanism (PA-20-185) ↗

See all 814 projects on NIH RePORTER →

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)

Grants.gov (RFA-CA-25-033) ↗Direct listing ↗Who already holds this grant ↗

RFA-FD-25-020Food and Drug Administrationcloses 05/16/2028

Reissue of RFA-FD-23-001- Clinical Studies of Orphan Products Addressing Unmet

Read announcement ↗Grants.gov (RFA-FD-25-020) ↗Direct listing ↗Who already holds this grant ↗

FOR-FD-25-020Food and Drug AdministrationForecast — not open yet

Clinical Studies of Orphan Products Addressing Unmet Needs of Rare Diseases (R

Grants.gov (FOR-FD-25-020) ↗Direct listing ↗Who already holds this grant ↗

FOR-FD-25-001Food and Drug AdministrationForecast — not open yet

Clinical Trials Addressing Unmet Needs of Rare Neurodegenerative Diseases (R01

Grants.gov (FOR-FD-25-001) ↗Direct listing ↗Who already holds this grant ↗

RFA-TR-25-002National Institutes of Healthcloses 07/02/2027

Preclinical Proof of Concept Studies for Rare Diseases (R21 Clinical Trial Not

Read announcement ↗Grants.gov (RFA-TR-25-002) ↗Direct listing ↗Who already holds this grant ↗

PAR-25-374National Institutes of Healthcloses 05/07/2028

Translational Bioinformatics and Experimental Approaches to Advance Drug Repos

Read announcement ↗Grants.gov (PAR-25-374) ↗Direct listing ↗Who already holds this grant ↗

HT942526PRCRPCTADefense Health Agency Contracting Activity -closes 10/05/2026

DoW Peer Reviewed Cancer, Clinical Trial Award

Grants.gov (HT942526PRCRPCTA) ↗Direct listing ↗Who already holds this grant ↗

PAR-26-049National Institutes of HealthForecast — not open yet

Establishing Pediatric CNS Pharmacodynamic Measures as Tools to Enable Psychia

Grants.gov (PAR-26-049) ↗Direct listing ↗Who already holds this grant ↗

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.

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.

Alembic Pharmaceuticals LtdChartwell Rx Sciences LlcHetero Labs Ltd Unit V

Manufacturers

companies with their own approval

Approved products

distinct strengths and forms

Routes

oral

2014

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.

← Back to the full ledger

What it's made of

Catechol

Where it can get to

What it binds — and whether we can reach it · 1 of 1 reachable

New uses, and who is already trying them

non-small cell lung carcinoma

cancer

head and neck squamous cell carcinoma

lung cancer

lung adenocarcinoma

Why nobody will fund it

What it would cost to find out

Ask for ideas nobody has listed

Who might pay for the trial

Who manufactures it

Closely related medicines