TACR1 tachykinin receptor 1
ENSG00000115353 · protein coding · Open Targets profile
Receptor for the tachykinin substance P, also able to bind and respond to tachynins neurokinin A/substance K and neurokinin B/neuromedin-K (PubMed:1718267, PubMed:15452552). The rank order of affinity of this receptor to tachykinins is: substance P > neurokinin A/substance K > neurokinin B/neuromedin-K (PubMed:1718267). Substance P binding to its receptor triggers G protein-coupled receptor signaling via activation of phosphatidylinositol hydrolysis by phospholipase C. Substance P binding also triggers signaling via activation of adenylate cyclase activity which results in increased intracellular levels of cyclic AMP (cAMP) (By similarity). {ECO:0000250|UniProtKB:P14600, ECO:0000269|PubMed:15452552, ECO:0000269|PubMed:1718267}.
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 Withdrawn means the drug was pulled from the market or from development.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, Structure with Ligand, High-Quality Ligand, High-Quality Pocket, Druggable Family
- Antibody
- GO CC high conf, UniProt loc med conf, UniProt SigP or TMHMM
- PROTAC
- Small Molecule Binder
gnomAD loss of function constraint: o/e 0.6983000040054321 (upper bound 0.9752799868583679). 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 100 registry trials, updated in the last three years, of the most advanced drugs against TACR1 (elinzanetant, fosaprepitant dimeglumine, aprepitant, rolapitant, fosaprepitant, fosnetupitant chloride, fosnetupitant, netupitant, serlopitant, tradipitant, ezlopitant, DNK333), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.
- Aimee RolstonUniversity of Michigan Rogel Cancer Center · 1 of 1 trials Phase 2+
- Alex MolasiotisUniversity of Derby · 1 of 1 trials Phase 2+
- Alice P ChenNational Cancer Institute (NCI) · 1 of 1 trials Phase 2+
- Benjamin FriedmanMontefiore Medical Center · 1 of 1 trials Phase 2+
- Benjamin W FriedmanMontefiore Medical Center · 1 of 1 trials Phase 2+
- Christian M BeilsteinBern University Hospital, University of Bern, Bern, Switzerland · 1 of 1 trials Phase 2+
- Chuangzhen ChenShantou University Medical College · 1 of 1 trials Phase 2+
- Detao YinThe First Affiliated Hospital of Zhengzhou University · 1 of 1 trials Phase 2+
- Emily LauMassachusetts General Hospital · 1 of 1 trials Phase 2+
- Fuming QiuSecond Affiliated Hospital, Zhejiang University, School of Medicine · 1 of 1 trials Phase 2+
- Gaétan PREVOSTUniversity Hospital, Rouen · 1 of 1 trials Phase 2+
- Jean-Christophe IANOTTOHématologie Clinique-Institut de Cancéro-Hématologie · 1 of 1 trials Phase 2+
- Jian ZhangPhase I Unit, Fudan University Shanghai Cancer Center, Shanghai, China · 1 of 1 trials Phase 2+
- Kathryn SchultzRush University Medical Center · 1 of 1 trials Phase 2+
- Kitty Clarence-SmithKM Pharmaceutical Consulting · 1 of 1 trials Phase 2+
Registry trials of elinzanetant, fosaprepitant dimeglumine, aprepitant, rolapitant, fosaprepitant, fosnetupitant chloride, fosnetupitant, netupitant, serlopitant, tradipitant, ezlopitant, DNK333 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; 75 of 86 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. 14 trials list no sites and are left out. Source: ClinicalTrials.gov, fetched live.
37 trials of drugs against TACR1 were stopped early; 2 give no reason
Terminated, withdrawn and suspended interventional trials of elinzanetant, fosaprepitant dimeglumine, aprepitant, rolapitant, fosaprepitant, fosnetupitant chloride, fosnetupitant, netupitant, serlopitant, tradipitant, ezlopitant, DNK333, 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 37.
- terminated · 2026-03-02 · Heron Therapeutics · Aprepitant injectable emulsion“Study was terminated early by Heron, and was not terminated for safety reasons.”
- terminated · 2025-06-18 · University of Michigan Rogel Cancer Center · matched by the registry's drug synonyms“Lack of Patient Population”
- terminated · 2025-05-04 · Helsinn Healthcare SA · Fosnetupitant 235 mg solution“Sponsor's decision”
- terminated · 2025-02-27 · Insel Gruppe AG, University Hospital Bern · Aprepitant 80 mg“Low recruiting rate”
- withdrawn · 2024-08-30 · University of Nebraska · aprepitant“It didn't get IRB approval.”
- withdrawn · 2024-08-07 · Australasian Leukaemia and Lymphoma Group · matched by the registry's drug synonyms“Study halted prematurely, prior to enrollment of first participant due to protracted logistical and subsequent funding matters.”
- terminated · 2024-05-14 · Vanda Pharmaceuticals · Tradipitant“Business Decision”
- terminated · 2023-11-13 · Albert Einstein College of Medicine · Aprepitant 125 mg, Fosaprepitant 115 MG“Expired IRB approval on 2/11/21”
- withdrawn · 2022-11-03 · Arun Gupta · Fosaprepitant“Alternate study commenced using different drug”
- terminated · 2021-08-09 · M.D. Anderson Cancer Center · Fosaprepitant Dimeglumine, Rolapitant Hydrochloride“Terminated per PI's request”
- terminated · 2021-05-20 · Vyne Therapeutics Inc. · Serlopitant“Business Reasons”
- terminated · 2021-05-20 · Vyne Therapeutics Inc. · 5 mg Serlopitant Tablets“No longer pursuing development of serlopitant”
- terminated · 2020-11-30 · Radboud University Medical Center · aprepitantNo reason given
- terminated · 2019-12-09 · Joseph Ma · Netupitant and Palonosetron“PI is leaving UCSD”
- terminated · 2019-10-09 · Sunnybrook Health Sciences Centre · Aprepitant“Study was stopped due to inadequate accrual.”
- withdrawn · 2019-05-22 · Costantine Albany · Rolapitant“Compound was sold by funder and development ceased.”
- terminated · 2019-03-15 · Merck Sharp & Dohme LLC · Fosaprepitant, Placebo for fosaprepitant“Further data are no longer required to support an application for use in pediatric patients. The decision to terminate was not based on any new safety findings”
- terminated · 2018-09-25 · Merck Sharp & Dohme LLC · Experimental: aprepitant, Experimental: fosaprepitant“Study terminated early prior to completing targeted enrollment of participants <6 months of age due to recruitment challenges.”
- terminated · 2018-08-27 · Merck Sharp & Dohme LLC · Fosaprepitant dimeglumine“Low enrollment”
- terminated · 2018-06-07 · St. Louis University · Fosaprepitant“Enrollment issues”
- terminated · 2018-05-22 · Gynecologic Oncology Group · Aprepitant“Study terminated due to no patient population available”
- terminated · 2017-11-17 · University of Southern California · fosaprepitant dimeglumine“Lack of Efficacy”
- terminated · 2017-05-18 · University of Washington · fosaprepitant dimeglumine“Study stopped due to lack of efficacy in first 6 patients”
- terminated · 2017-05-10 · Vanderbilt University Medical Center · Aprepitant“Difficulty recruiting.”
- terminated · 2017-05-09 · OHSU Knight Cancer Institute · fosaprepitant dimeglumine“Drug contract timelines and inadequate enrollment”
Paediatric incentives and obligations for TACR1's drugs
For elinzanetant, fosaprepitant dimeglumine, aprepitant, rolapitant, fosaprepitant, fosnetupitant chloride, fosnetupitant, netupitant, serlopitant, tradipitant, ezlopitant, DNK333: 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 · TACR1 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 · EMEA-001198-PIP04-23 (netupitant;palonosetron, Prevention of chemotherapy-induced nausea and vomiting): W: decision granting a waiver in all age groups for all conditions or indications, 4 Dec 2024; EMEA-003500-PIP01-23 (elinzanetant, Treatment of vasomotor symptoms caused by endocrine therapy related to breast cancer): W: decision granting a waiver in all age groups for all conditions or indications, 29 Dec 2023; EMEA-001198-PIP03-17-M05 (Fosnetupitant;palonosetron, Prevention of chemotherapy-induced nausea and vomiting): PM: decision on the application for modification of an agreed PIP, 25 Oct 2023; EMEA-001768-PIP02-15-M03 (rolapitant, Prevention of nausea and vomiting): W: decision granting a waiver in all age groups for all conditions or indications, 15 May 2020; +5 moreRule: 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: no · No EU orphan designation names elinzanetant, fosaprepitant dimeglumine, aprepitant, rolapitant, fosaprepitant, fosnetupitant chloride, fosnetupitant, netupitant, serlopitant, tradipitant, ezlopitant, dnk333Rule: 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: yes · Lynkuet: authorised since 17 Nov 2025; Akynzeo: authorised since 27 May 2015; Ivemend: authorised since 11 Jan 2008; Emend: authorised since 11 Nov 2003; +1 moreRule: 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 elinzanetant, fosaprepitant dimeglumine, aprepitant, rolapitant, fosaprepitant, fosnetupitant chloride, fosnetupitant, netupitant, serlopitant, tradipitant, ezlopitant, dnk333Rule: FDA's Pediatric Oncology Drug Approvals table names the drug. Source: FDA Pediatric Oncology Drug Approvals (content current as of 2026-03-03), 2026-11-12
- Registered studies open to children: yes · 33 interventional studies of elinzanetant, fosaprepitant dimeglumine, aprepitant, rolapitant, fosaprepitant, fosnetupitant chloride, fosnetupitant, netupitant, serlopitant, tradipitant, ezlopitant, dnk333 include patients under 18; 3 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, 2026-11-12
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 19 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.