S1PR1 sphingosine-1-phosphate receptor 1
ENSG00000170989 · protein coding · Open Targets profile
G protein-coupled receptor for the bioactive lysosphingolipid sphingosine 1-phosphate (S1P) that seems to be coupled to the G(i) subclass of heteromeric G proteins. Signaling leads to the activation of RAC1, SRC, PTK2/FAK1 and MAP kinases. Plays an important role in cell migration, probably via its role in the reorganization of the actin cytoskeleton and the formation of lamellipodia in response to stimuli that increase the activity of the sphingosine kinase SPHK1. Required for normal chemotaxis toward sphingosine 1-phosphate. Required for normal embryonic heart development and normal cardiac morphogenesis. Plays an important role in the regulation of sprouting angiogenesis and vascular maturation. Inhibits sprouting angiogenesis to prevent excessive sprouting during blood vessel development. Required for normal egress of mature T-cells from the thymus into the blood stream and into peripheral lymphoid organs. Plays a role in the migration of osteoclast precursor cells, the regulation of bone mineralization and bone homeostasis (By similarity). Plays a role in responses to oxidized 1-palmitoyl-2-arachidonoyl-sn-glycero-3- phosphocholine by pulmonary endothelial cells and in the protection against ventilator-induced lung injury. {ECO:0000250, ECO:0000269|PubMed:10982820, ECO:0000269|PubMed:11230698, ECO:0000269|PubMed:11583630, ECO:0000269|PubMed:11604399, ECO:0000269|PubMed:19286607, ECO:0000269|PubMed:22344443, ECO:0000269|PubMed:8626678, ECO:0000269|PubMed:9488656}.
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 Withdrawn means the drug was pulled from the market or from development.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, Druggable Family
- Antibody
- UniProt loc high conf, GO CC high conf, UniProt SigP or TMHMM
- PROTAC
- Database Ubiquitination, Small Molecule Binder
gnomAD loss of function constraint: o/e 0.10903000086545944 (upper bound 0.34321001172065735). 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 88 registry trials, updated in the last three years, of the most advanced drugs against S1PR1 (siponimod, etrasimod, ponesimod, etrasimod arginine, ozanimod, fingolimod lauryl, siponimod fumaric acid, fingolimod, cenerimod, mocravimod, amiselimod), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.
- Bristol-Myers SquibbBristol-Myers Squibb · 9 of 9 trials Phase 2+
- Bart RypmaThe University of Texas at Dallas · 1 of 1 trials Phase 2+
- Boris DecourtTexas Tech University Health Sciences Center · 1 of 1 trials Phase 2+
- Daniel OntanedaThe Cleveland Clinic · 1 of 1 trials Phase 2+
- Daniele D'AmbrosioActelion · 1 of 1 trials Phase 2+
- David MarsolaisCRIUCPQ-UL · 1 of 1 trials Phase 2+
- Enrique AlvarezUniversity of Colorado, Denver · 1 of 1 trials Phase 2+
- François LelloucheIUCPQ-UL · 1 of 1 trials Phase 2+
- Geert DHaensAmsterdamUMC · 1 of 1 trials Phase 2+
- Harriet KlugerYale University · 1 of 1 trials Phase 2+
- HuiSheng ChenThe General Hospital of Northern Theater Command · 1 of 1 trials Phase 2+
- John LaheyBausch Health Americas, Inc. · 1 of 1 trials Phase 2+
- Kaichun WuThe First Affiliated Hospital of Fourth Military Medical University, PLA · 1 of 1 trials Phase 2+
- Marcos DeLimaThe Ohio State University Comprehensive Cancer Center · 1 of 1 trials Phase 2+
- Marwan N SabbaghSt. Josep's Hospital and Medical Center, Phoenix · 1 of 1 trials Phase 2+
Registry trials of siponimod, etrasimod, ponesimod, etrasimod arginine, ozanimod, fingolimod lauryl, siponimod fumaric acid, fingolimod, cenerimod, mocravimod, amiselimod 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; 43 of 84 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. 4 trials list no sites and are left out. Source: ClinicalTrials.gov, fetched live.
43 trials of drugs against S1PR1 were stopped early; 6 give no reason
Terminated, withdrawn and suspended interventional trials of siponimod, etrasimod, ponesimod, etrasimod arginine, ozanimod, fingolimod lauryl, siponimod fumaric acid, fingolimod, cenerimod, mocravimod, amiselimod, 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 43.
- terminated · 2026-07-01 · Pfizer · Etrasimod“The study was prematurely discontinued due to a lack of efficacy in sub-study 1”
- terminated · 2026-02-10 · Bristol-Myers Squibb · Ozanimod“Business objectives have changed.”
- withdrawn · 2026-01-14 · Yale University · Etrasimod“The study was terminated early as no patients were enrolled.”
- withdrawn · 2025-12-02 · Bristol-Myers Squibb · matched by the registry's drug synonyms“Replaced with another clinical trial”
- terminated · 2025-11-04 · Celgene · Ozanimod“Business objectives have changed.”
- terminated · 2025-10-09 · Celgene · Ozanimod“The study has terminated due to non-safety reasons; Business Objectives have changed.”
- terminated · 2025-09-17 · Celgene · Ozanimod“Business objectives have changed”
- withdrawn · 2025-08-17 · University Hospital, Antwerp · matched by the registry's drug synonyms“Feasibility issues, insufficient funding, delays due transition to CTIS.”
- terminated · 2025-06-12 · Celgene · matched by the registry's drug synonyms“Business objective has changed”
- terminated · 2025-05-13 · State University of New York at Buffalo · matched by the registry's drug synonyms“Lack of recruitment”
- terminated · 2025-05-08 · Pfizer · etrasimod“Per the results of the planned interim analysis, the study met futility criteria for efficacy so the trial was terminated. This decision was made for efficacy reasons only and is not due to any safety concerns.”
- terminated · 2025-04-22 · Bristol-Myers Squibb · Ozanimod“Study was terminated due to business reasons.”
- terminated · 2025-03-26 · Bristol-Myers Squibb · Ozanimod“Business objectives have changed”
- terminated · 2025-02-04 · Actelion · Ponesimod“Low recruitment”
- terminated · 2025-01-15 · I.R.C.C.S. Fondazione Santa Lucia · Ozanimod Oral Capsule“Sponsor's decision”
- withdrawn · 2024-09-19 · Geert D'Haens · Ozanimod Oral Capsule“Funder decision”
- withdrawn · 2024-08-09 · The University of Texas at Dallas · Ozanimod“The funding for the study was revoked. As such, the study is no longer being conducted.”
- terminated · 2024-02-20 · Centre de Recherche de l'Institut Universitaire de Cardiologie et de Pneumologie de Quebec · Ozanimod“Screening was stopped by the Sponsor (43/48 participants enrolled), given the very low number of eligible patients (high vaccination rate and occurrence of the Omicron variant). The last patient randomized performed his follow-up visit.”
- terminated · 2022-03-24 · Arena Pharmaceuticals · matched by the registry's drug synonyms“Sponsor decision”
- terminated · 2021-07-29 · Charite University, Berlin, Germany · matched by the registry's drug synonyms“delayed recruitment”
- withdrawn · 2021-07-22 · Second Affiliated Hospital, Zhejiang University, School of Medicine · FingolimodNo reason given
- terminated · 2021-06-11 · Arena Pharmaceuticals · matched by the registry's drug synonyms“Terminated [Sponsor decision to terminate the study]”
- terminated · 2021-05-18 · Actelion · Ponesimod“sponsor decision due to low recruitment”
- terminated · 2021-01-05 · Novartis Pharmaceuticals · matched by the registry's drug synonyms“The study was terminated prematurely after an interim analysis for futility. The study did not provide any evidence for efficacy of BAF312 in dermatomyositis.”
- terminated · 2021-01-05 · Novartis Pharmaceuticals · matched by the registry's drug synonymsNo reason given
Paediatric incentives and obligations for S1PR1's drugs
For siponimod, etrasimod, ponesimod, etrasimod arginine, ozanimod, fingolimod lauryl, siponimod fumaric acid, fingolimod, cenerimod, mocravimod, amiselimod: 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 · S1PR1 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/0000184081 (etrasimod, Treatment of ulcerative colitis): PM: decision on the application for modification of an agreed PIP, 3 Jan 2025; EMEA-001710-PIP04-17-M03 (Ozanimod (hydrochloride), Treatment of Crohn's disease): PM: decision on the application for modification of an agreed PIP, 13 Apr 2022; EMEA-002713-PIP02-21-M02 (etrasimod, Treatment of Crohn's disease): PM: decision on the application for modification of an agreed PIP, 13 Sept 2024; EMEA-003304-PIP01-22 (mocravimod, Treatment in haematopoietic stem cell transplantation in patients with acute myeloid leukaemia): P: decision agreeing on a investigation plan, with or without partial waiver(s) and or deferral(s), 7 Aug 2023; +6 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: yes · EU/3/23/2776 positive 22 May 2023: Treatment of hypomyelinating leukodystrophy-18; EU/3/21/2520 positive 12 Nov 2021: Treatment of adrenoleukodystrophy; EU/3/21/2504 positive 15 Oct 2021: Treatment in haematopoietic stem cell transplantation; EU/3/14/1369 withdrawn 19 Nov 2014: Treatment of dermatomyositis; +2 moreRule: 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 · Fingolimod Accord: authorised since 25 Jun 2020; Gilenya: authorised since 17 Mar 2011; Velsipity: authorised since 16 Feb 2024; Mayzent: authorised since 13 Jan 2020; +4 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 siponimod, etrasimod, ponesimod, etrasimod arginine, ozanimod, fingolimod lauryl, siponimod fumaric acid, fingolimod, cenerimod, mocravimod, amiselimodRule: 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 · 18 interventional studies of siponimod, etrasimod, ponesimod, etrasimod arginine, ozanimod, fingolimod lauryl, siponimod fumaric acid, fingolimod, cenerimod, mocravimod, amiselimod include patients under 18; 11 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 14 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.