TLR7 toll like receptor 7
ENSG00000196664 · protein coding · Open Targets profile
Endosomal receptor that plays a key role in innate and adaptive immunity (PubMed:14976261, PubMed:32433612). Controls host immune response against pathogens through recognition of uridine- containing single strand RNAs (ssRNAs) of viral origin or guanosine analogs (PubMed:12738885, PubMed:27742543, PubMed:31608988, PubMed:32706371, PubMed:35477763). Upon binding to agonists, undergoes dimerization that brings TIR domains from the two molecules into direct contact, leading to the recruitment of TIR-containing downstream adapter MYD88 through homotypic interaction (PubMed:27742543). In turn, the Myddosome signaling complex is formed involving IRAK4, IRAK1, TRAF6, TRAF3 leading to activation of downstream transcription factors NF-kappa-B and IRF7 to induce pro-inflammatory cytokines and interferons, respectively (PubMed:27742543, PubMed:32706371). In plasmacytoid dendritic cells, RNASET2 endonuclease cooperates with PLD3 or PLD4 5'->3' exonucleases to process RNA and release 2',3'-cyclic guanosine monophosphate (2',3'-cGMP) and cytidine-rich RNA fragments that occupy TLR7 ligand-binding pockets and trigger a signaling- competent state. {ECO:0000269|PubMed:12738885, ECO:0000269|PubMed:14976261, ECO:0000269|PubMed:27742543, ECO:0000269|PubMed:31608988, ECO:0000269|PubMed:32433612, ECO:0000269|PubMed:32706371, ECO:0000269|PubMed:35477763, ECO:0000269|PubMed:38697119}.
Each band is a group of drugs. It runs from the kind of drug on the left to the furthest stage that drug has reached in any disease on the right. Thicker bands mean more drugs.
Approved bands are highlighted. Withdrawn means the drug was pulled from the market or from development. A combined phase counts as the later one (Phase 1/2 is shown as Phase 2). Hover a band for the drug names. Source: Open Targets Platform, fetched live.
Each row is a cancer, strongest overall evidence first. The two dots show how strong the inherited (germline) and tumour-mutation (somatic) evidence is; the line between them is the gap.
Scores run from 0 (no evidence) to 1 (strongest). A missing dot at 0 means Open Targets holds no evidence of that kind. Source: Open Targets Platform, fetched live.
Tractability
- Small molecule
- Approved Drug, High-Quality Ligand, Druggable Family
- Antibody
- GO CC high conf, UniProt SigP or TMHMM
- PROTAC
- Database Ubiquitination, Half-life Data, Small Molecule Binder
- Other modalities
- Advanced Clinical
gnomAD loss of function constraint: o/e 0.31327998638153076 (upper bound 0.5075700283050537). Low values mean loss of function is poorly tolerated, a safety flag for inhibition.
Who runs trials of these drugs
Principal investigators and study chairs on 196 registry trials, updated in the last three years, of the most advanced drugs against TLR7 (hydroxychloroquine, enpatoran, CPG-52852, bazlitoran, vesatolimod, resiquimod, afimetoran, GSK-2245035, AZD-8848), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.
- Angela DeMicheleUniversity of Pennsylvania · 2 of 2 trials Phase 2+
- Jing HePeking University People's Hospital · 2 of 2 trials Phase 2+
- Sabine HazanProgenaBiome · 2 of 2 trials Phase 2+
- Sukeshi Patel AroraCancer Therapy & Research Center University of Texas Health Science Center San Antonio · 2 of 2 trials Phase 2+
- Ahmed M SayedAljazeera (Al Gazeera) hospital · 1 of 1 trials Phase 2+
- Alfredo Hernandez-RuizClinica Somer · 1 of 1 trials Phase 2+
- Amadou A. SallInstitut Pasteur de Dakar, Senegal · 1 of 1 trials Phase 2+
- Amy ClarkAbramson Cancer Center at Penn Medicine · 1 of 1 trials Phase 2+
- Anbin HuangUnion Hospital, Tongji Medical College, Huazhong University of Science and Technology · 1 of 1 trials Phase 2+
- Anthony JoshuaSt Vincent's Hospital, Sydney · 1 of 1 trials Phase 2+
- Arsène MEKINIANInternal Medecine_Hospital Saint Antoine · 1 of 1 trials Phase 2+
- Ashutosh M. ShuklaNorth Florida/South Georgia Veterans Health System, Gainesville, FL · 1 of 1 trials Phase 2+
- Assoc. Prof. Levent ĞANAYUniversity of Health Sciences Istanbul Ümraniye Training and Research Hospital · 1 of 1 trials Phase 2+
- Austin DuffyMater Misericordiae University Hospital · 1 of 1 trials Phase 2+
- BERNARD BELAIGUESAssistance Publique hôpitaux de Marseille · 1 of 1 trials Phase 2+
Registry trials of hydroxychloroquine, enpatoran, CPG-52852, bazlitoran, vesatolimod, resiquimod, afimetoran, GSK-2245035, AZD-8848 updated in the last three years, counted by the country group of their listed sites. A trial with sites in several groups counts in each; 169 of 189 have all sites in one country.
Site counts are not patients per country, and trials registered only outside ClinicalTrials.gov are not covered. Where sites are is a fact about the record, not a judgement of its quality. Europe is the EU and EEA, the UK and Switzerland. 7 trials list no sites and are left out. Source: ClinicalTrials.gov, fetched live.
157 trials of drugs against TLR7 were stopped early; 1 give no reason
Terminated, withdrawn and suspended interventional trials of hydroxychloroquine, enpatoran, CPG-52852, bazlitoran, vesatolimod, resiquimod, afimetoran, GSK-2245035, AZD-8848, telratolimod, newest update first, live from ClinicalTrials.gov. Each reason is quoted exactly as the registry gives it; we do not sort reasons into safety, efficacy or business. Dates are the last registry update. Showing the 25 most recent of 157.
- terminated · 2026-10-19 · Duke University · matched by the registry's drug synonyms“Adjuvant stability not extended”
- terminated · 2026-10-06 · ECOG-ACRIN Cancer Research Group · Hydroxychloroquine“Slow accrual”
- terminated · 2026-09-09 · EMD Serono Research & Development Institute, Inc. · matched by the registry's drug synonyms“Based on interim analyses for futility”
- withdrawn · 2026-09-08 · Apsen Farmaceutica S.A. · Hydroxychloroquine Sulfate, Hydroxychloroquine Sulfate + Azythromycin“This study was canceled before enrollment due to a decision by the Sponsor”
- suspended · 2026-09-02 · National Institute of Allergy and Infectious Diseases (NIAID) · Vesatolimod (VES)“Temporarily Closed (Paused) to Accrual and Study Agents/Products”
- terminated · 2026-07-20 · National Institute of Allergy and Infectious Diseases (NIAID) · matched by the registry's drug synonyms“The study is being closed early due to insufficient participant enrollment across study sites.”
- terminated · 2026-06-12 · Northwestern University · Hydroxychloroquine in Combination With Encorafenib and Cetuximab or Panitumumab“The study was closed due to accrual.”
- withdrawn · 2026-05-19 · Nicholas Carlson · Hydroxychloroquine“No funding”
- terminated · 2026-05-14 · University of Utah · Hydroxychloroquine“Lack of Funding”
- terminated · 2026-04-29 · Guy's and St Thomas' NHS Foundation Trust · Hydroxychloroquine“Recruitment was terminated early by the funder due to study sites' inability to recruit sufficient number of participants.”
- terminated · 2026-04-14 · University Hospital, Rouen · Hydroxychloroquine“Difficulty in enrolling new patients”
- terminated · 2026-04-13 · Cancer Trials Ireland · Hydroxychloroquine“Study terminated due to futility”
- withdrawn · 2026-04-06 · Assistance Publique - Hôpitaux de Paris · matched by the registry's drug synonyms“The study was terminated following revisions to the diagnostic criteria defining the target pathology, which significantly impacted the study design”
- terminated · 2026-03-27 · Incannex Healthcare Ltd · Hydroxychloroquine“Recruitment challenges”
- suspended · 2026-03-03 · National Institute of Allergy and Infectious Diseases (NIAID) · matched by the registry's drug synonyms“Temporarily Closed (paused)”
- terminated · 2026-02-06 · Queen's Medical Center · Hydroxychloroquine“RECOVERY Trial results - no efficacy”
- terminated · 2025-12-03 · Matthias Griese · Hydroxychloroquine sulfate“Lack of ressources after inspection and appropriate correcting actions to be taken”
- terminated · 2025-09-25 · BioMed Valley Discoveries, Inc · Hydroxychloroquine“Lack of Enrollment for Remaining Open Baskets”
- terminated · 2025-09-23 · Sanofi · Hydroxychloroquine SAR321068“Rate of enrollment too slow to allow completion in a reasonable timeframe”
- withdrawn · 2025-09-15 · London Health Sciences Centre Research Institute OR Lawson Research Institute of St. Joseph's · Hydroxychloroquine“Study Withdrawn”
- suspended · 2025-09-04 · National Institute of Allergy and Infectious Diseases (NIAID) · matched by the registry's drug synonyms“Temporarily Closed (Paused) to Accrual”
- terminated · 2025-06-12 · National Institute of Allergy and Infectious Diseases (NIAID) · Hydroxychloroquine“Enrollment was closed before reaching the target. In the 1st interim analysis after enrollment closure, the follow up \& treatment of active participants were stopped early due to evidence of futility.”
- withdrawn · 2025-05-16 · Memorial Sloan Kettering Cancer Center · Hydroxychloroquine“Emerging evidence does not support the use of HCQ for treatment or prevention of SARS -CoV2 infection. No pts have been enrolled.”
- withdrawn · 2025-03-26 · National Institute of Allergy and Infectious Diseases (NIAID) · matched by the registry's drug synonyms“FDA Clinical Hold”
- terminated · 2025-03-10 · Istituto Romagnolo per lo Studio dei Tumori Dino Amadori IRST S.r.l. IRCCS · Hydroxychloroquine“Difficulties in recruiting subjects were observed soon after the study was initiated. This difficulty was attributed to the decreased incidence of infections which occurred in the period following the first lock down.”
Paediatric incentives and obligations for TLR7's drugs
For hydroxychloroquine, enpatoran, CPG-52852, bazlitoran, vesatolimod, resiquimod, afimetoran, GSK-2245035, AZD-8848, telratolimod: what EMA and FDA publish about paediatric plans, orphan status and pediatric approvals, and how many registered studies take children. Each line is a yes, no or not published fact from the record linked under it; none of it is a forecast.
- FDA pediatric target list: no · TLR7 is not on the listRule: Target is on FDA's Pediatric Molecular Target List (relevant targets). Source: FDA Pediatric Molecular Target List (Listed as February 2026 on the FDA Pediatric Oncology page; the file served is 9.7.22_the_relevant_molecular_target_list.xlsx, whose Summary of Changes sheet is headed 'SEPTEMBER 2022 UPDATE' (footnote date 2022-09-01)), 2026-11-11
- EU paediatric investigation plan: yes · EMA/PE/0000181238 (resiquimod, Treatment of melanoma): P: decision agreeing on a investigation plan, with or without partial waiver(s) and or deferral(s), 6 Dec 2024; EMEA-003342-PIP02-22 (Enpatoran, Treatment of Systemic Lupus Erythematosus (SLE)): P: decision agreeing on a investigation plan, with or without partial waiver(s) and or deferral(s), 27 Oct 2023; EMEA-003342-PIP01-22 (Enpatoran, Treatment of cutaneous lupus erythemathosus): W: decision granting a waiver in all age groups for all conditions or indications, 10 Mar 2023Rule: An EMA PIP decision (agreement, modification or waiver) lists the drug as its active substance, exact name. Source: EMA data download (dated snapshot), 2026-11-11
- EU orphan designation: yes · EU/3/16/1653 positive 28 Apr 2016: Treatment of cutaneous T-cell lymphoma; EU/3/16/1820 positive 12 Jan 2017: Treatment of antiphospholipid syndrome; EU/3/17/1963 positive 8 Oct 2009: Treatment of LIPIN1 diseaseRule: An EU orphan designation lists the drug as its active substance (exact name) or belongs to a medicine that does; withdrawn and expired designations are listed with their status. Source: EMA data download (dated snapshot), 2026-11-11
- Authorised in the EU: no · EMA lists no centrally authorised medicine of hydroxychloroquine, enpatoran, cpg-52852, bazlitoran, vesatolimod, resiquimod, afimetoran, gsk-2245035, azd-8848, telratolimodRule: An EMA medicine record lists the drug as its active substance or INN, exact name; national-only authorisations are not in this file. Source: EMA data download (dated snapshot), 2026-11-11
- FDA orphan designation: not published · FDA's orphan designation database turns away automated requests, so this app does not read it; search it by hand at the linkRule: Would be: an FDA orphan designation names the drug. Source: FDA orphan designations search
- FDA pediatric oncology approval: no · FDA's table lists no pediatric approval of hydroxychloroquine, enpatoran, cpg-52852, bazlitoran, vesatolimod, resiquimod, afimetoran, gsk-2245035, azd-8848, telratolimodRule: FDA's Pediatric Oncology Drug Approvals table names the drug. Source: FDA Pediatric Oncology Drug Approvals (content current as of 2026-03-03), 2026-11-11
- Registered studies open to children: yes · 56 interventional studies of hydroxychloroquine, enpatoran, cpg-52852, bazlitoran, vesatolimod, resiquimod, afimetoran, gsk-2245035, azd-8848, telratolimod include patients under 18; 14 are recruiting, not yet recruiting or activeRule: The registry's age group includes Child (birth to 17 years), which also counts studies that set no minimum age. Source: ClinicalTrials.gov search, 2026-11-11
Rare pediatric disease voucher. FDA, content current as of 29 Apr 2026: “As of February 3, 2026, enactment of the Consolidated Appropriations Act, 2026, the rare pediatric disease PRV program will sunset after September 30, 2029. FDA may not award any PRVs under this program after September 30, 2029.” Voucher sale prices are not shown here; they appear only as company-reported news. FDA: Rare Pediatric Disease Designation and Priority Review Voucher Programs
All 12 drugs and clinical candidates as a table
Each drug, stage and indication links to its Open Targets record, where the trials and approvals behind it are listed. Salt forms (for example a mesylate) are listed as Open Targets records them, as separate entries.