Study of Tilpisertib Fosmecarbil in Participants With Moderately to Severely Active Ulcerative Colitis
PALEKONA
A Phase 2, Double-Blinded, Randomized, Placebo-Controlled, Dose-Ranging Study Evaluating the Efficacy and Safety of GS-5290 in Participants With Moderately to Severely Active Ulcerative Colitis
3 other identifiers
interventional
176
13 countries
98
Brief Summary
The goal of this study is to learn if tilpisertib fosmecarbil (formerly known as GS-5290) is effective and safe in treating participants with moderate to severe ulcerative colitis. The study will compare participants in different treatment groups treated with tilpisertib fosmecarbil with participants treated with placebo. The primary objective of this study is to demonstrate the efficacy of tilpisertib fosmecarbil, compared to placebo control, in achieving Clinical Response at Week 12.
Trial Health
Trial Health Score
Automated assessment based on enrollment pace, timeline, and geographic reach
participants targeted
Target at P75+ for phase_2
Started Dec 2023
Typical duration for phase_2
98 active sites
Health score is calculated from publicly available data and should be used for screening purposes only.
Trial Relationships
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Study Timeline
Key milestones and dates
First Submitted
Initial submission to the registry
September 1, 2023
CompletedFirst Posted
Study publicly available on registry
September 8, 2023
CompletedStudy Start
First participant enrolled
December 5, 2023
CompletedPrimary Completion
Last participant's last visit for primary outcome
January 1, 2027
ExpectedStudy Completion
Last participant's last visit for all outcomes
February 1, 2028
September 11, 2026
September 1, 2026
3.1 years
September 1, 2023
September 9, 2026
Conditions
Outcome Measures
Primary Outcomes (1)
Proportion of Participants Achieving Clinical Response Per Modified Mayo Clinic Score at Week 12
Clinical Response is defined as a decrease from baseline of ≥ 2 points and at least 30% in 3 components of the modified Mayo Clinic Score, Stool Frequency, Rectal Bleeding, and Endoscopic Findings, in addition to a ≥ 1 point decrease from baseline in the Rectal Bleeding subscore or Rectal Bleeding subscore of ≤ 1. The modified Mayo Clinic Score is a scoring system for assessment of UC activity and is composed of subscores from endoscopy (range: 0 to 3, where 0 = normal or inactive disease and 3 = severe disease \[spontaneous bleeding, ulceration\]), rectal bleeding (range: 0 to 3, where 0 = no blood seen and 3 = blood alone passes), and stool frequency (range: 0 to 3, where 0 = normal number of stools and 3 = at least 5 or more stools more than normal). Total score for modified Mayo Clinic Score ranges from 0 to 9 (sum of all subscores), with higher scores indicating higher disease activity.
Week 12
Secondary Outcomes (5)
Proportion of Participants Achieving Clinical Remission Per Modified Mayo Clinic Score at Week 12
Week 12
Proportion of Participants Achieving Endoscopic Response at Week 12
Week 12
Proportion of Participants Achieving Histologic Endoscopic Mucosal Improvement at Week 12
Week 12
Percentage of Participants Experiencing Treatment-emergent Adverse Events (TEAEs)
First dose date up to Week 52 (responders) or Week 64 (non-responders) plus 30 days
Percentage of Participants Experiencing Clinically Significant Laboratory Abnormalities
First dose date up to Week 52 (responders) or Week 64 (non-responders) plus 30 days
Study Arms (4)
Tilpisertib Fosmecarbil Dose A
EXPERIMENTALBlinded Treatment Phase: Participants will receive tilpisertib fosmecarbil Dose A for up to 12 weeks. An efficacy assessment will be performed at Week 12. • Participants who achieve clinical response will receive tilpisertib fosmecarbil Dose B for up to Week 52. Non-responder Treatment Phase: • Participants who do not achieve clinical response at Week 12 will discontinue the Blinded Treatment Phase and have the option to enter into the Non-responder Treatment Phase. Participants will receive tilpisertib fosmecarbil Dose A for another 12 weeks. An efficacy assessment will be performed at Week 12 of the Non-responder Treatment Phase. Participants who achieved clinical response will receive tilpisertib fosmecarbil Dose B for up to Week 52. Participants who do not achieve clinical response at Non-responder Treatment Phase Week 12 will discontinue study drug.
Tilpisertib Fosmecarbil Dose B
EXPERIMENTALBlinded Treatment Phase: Participants will receive tilpisertib fosmecarbil Dose B for up to 12 weeks. An efficacy assessment will be performed at Week 12. • Participants who achieve clinical response will receive tilpisertib fosmecarbil Dose B for up to Week 52. Non-responder Treatment Phase: • Participants who do not achieve clinical response at Week 12 will discontinue the Blinded Treatment Phase and have the option to enter into the Non-responder Treatment Phase. Participants will receive tilpisertib fosmecarbil Dose B for another 12 weeks. An efficacy assessment will be performed at Week 12 of the Non-responder Treatment Phase. Participants who achieved clinical response will receive tilpisertib fosmecarbil Dose B for up to Week 52. Participants who do not achieve clinical response at Non-responder Treatment Phase Week 12 will discontinue study drug.
Tilpisertib Fosmecarbil Dose C
EXPERIMENTALBlinded Treatment Phase: Participants will receive tilpisertib fosmecarbil Dose C for up to 12 weeks. An efficacy assessment will be performed at Week 12. • Participants who achieve clinical response will receive tilpisertib fosmecarbil Dose C for up to Week 52. Non-responder Treatment Phase: • Participants who do not achieve clinical response at Week 12 will discontinue the Blinded Treatment Phase and have the option to enter into the Non-responder Treatment Phase. Participants will receive tilpisertib fosmecarbil Dose B for another 12 weeks. An efficacy assessment will be performed at Week 12 of the Non-responder Treatment Phase. Participants who achieved clinical response will receive tilpisertib fosmecarbil Dose B for up to Week 52. Participants who do not achieve clinical response at Non-responder Treatment Phase Week 12 will discontinue study drug.
Tilpisertib Fosmecarbil Placebo
PLACEBO COMPARATORBlinded Treatment Phase: Participants will receive tilpisertib fosmecarbil placebo for up to 12 weeks. An efficacy assessment will be performed at Week 12. • Participants who achieve clinical response will receive tilpisertib fosmecarbil Dose C for up to Week 52. Non-responder Treatment Phase: • Participants who do not achieve clinical response at Week 12 will discontinue the Blinded Treatment Phase and have the option to enter into the Non-responder Treatment Phase. Participants will receive tilpisertib fosmecarbil Dose A for another 12 weeks. An efficacy assessment will be performed at Week 12 of the Non-responder Treatment Phase. Participants who achieved Clinical Response will receive tilpisertib fosmecarbil Dose B for up to Week 52. Participants who do not achieve Clinical Response at Non-responder Treatment Phase Week 12 will discontinue study drug.
Interventions
Tablets administered orally
Eligibility Criteria
You may qualify if:
- Individuals assigned male at birth, or nonpregnant, nonlactating individuals assigned female at birth, 18 to 75 years of age based on the date of the screening visit.
- Ulcerative colitis (UC) of at least 90-day duration before randomization confirmed by endoscopy and histology at any time in the past AND a minimum disease extent of 15 cm from the anal verge. Documentation of endoscopy and histology consistent with the diagnosis of UC must be available in the source documents prior to the initiation of screening.
- Moderately to severely active UC as determined during screening with a modified Mayo Clinic Score based on the sum of Stool Frequency, Rectal Bleeding, and Endoscopic Finding of 5 to 9 points and an endoscopic subscore of 2 to 3 (determined by central reader).
- Previous treatment history of approved UC therapy with at least one advanced therapy mechanisms of action but failure (ie, loss of response or lack of response) of no more than 3 different advanced therapy mechanisms of action.
- A surveillance colonoscopy for dysplasia is required prior to randomization if indicated by regional guidelines for individuals with UC.
You may not qualify if:
- Current diagnosis of Crohn's Disease (CD) or diagnosis of indeterminate colitis due to an enteric pathogen, lymphocytic or collagenous colitis.
- Individuals with disease limited to the rectum (ulcerative proctitis) during screening endoscopy.
- Requirement for ongoing therapy with or prior use of any prohibited medications.
- Active clinically significant infection, or any infection requiring hospitalization or treatment with intravenous anti-infectives within 8 weeks.
- of randomization; or any infection requiring oral anti-infective therapy within 6 weeks of randomization.
- History of opportunistic infection.
- Current diagnosis of acute severe colitis, fulminant colitis, or toxic megacolon.
Contact the study team to confirm eligibility.
Sponsors & Collaborators
- Gilead Scienceslead
Study Sites (102)
GI Alliance
Sun City, Arizona, 85351, United States
GastroSb Weight Loss Clinic
Chula Vista, California, 91910, United States
Southern California Research Centers
Coronado, California, 92118, United States
VVCRD Research
Garden Grove, California, 92845, United States
UC San Diego Health System
La Jolla, California, 92037, United States
Gastro Care Institute
Lancaster, California, 93534, United States
Om Research LLC
Lancaster, California, 93534, United States
University of California, Davis
Sacramento, California, 95817, United States
University of California San Francisco
San Francisco, California, 94115, United States
Luna Research
Coral Gables, Florida, 33134, United States
University of Florida
Gainesville, Florida, 32610, United States
The Medici Medical Research
Hollywood, Florida, 33021, United States
Clinical Research of Osceola
Kissimmee, Florida, 34741, United States
Florida Research Institute
Largo, Florida, 33771, United States
GI PROS Research
Naples, Florida, 34102, United States
Clinical One Research
Orlando, Florida, 32807, United States
Digestive and Liver Center of Florida, LLC
Orlando, Florida, 32825, United States
Advanced Medical Research Center
Port Orange, Florida, 32127, United States
Corewell Health
Grand Rapids, Michigan, 49546, United States
Mayo Clinic
Rochester, Minnesota, 55905, United States
Gastroenterology Associates of North Mississippi
Oxford, Mississippi, 38655, United States
Digestive Health Specialists
Tupelo, Mississippi, 38801, United States
St. Charles Clinical Research
St Louis, Missouri, 63141, United States
NYU Langone Long Island Clinical Research Associates
Great Neck, New York, 11021, United States
Gastroenterology & Hepatology Specialists Inc
Canton, Ohio, 44718, United States
The Ohio State University Wexner Medical Centre
Columbus, Ohio, 43210, United States
Skyline Gastroenterology of West Tennessee
Jackson, Tennessee, 38301, United States
Gastroenterology Research of Hill Country
Boerne, Texas, 78006, United States
GI Alliance
Lubbock, Texas, 79410, United States
Clinical Associates in Research Therapeutics of America
San Antonio, Texas, 78212, United States
Gastroenterology Research of San Antonio
San Antonio, Texas, 78229, United States
Tyler Research Institute, LLC
Tyler, Texas, 75701, United States
Gastroenterology Associates of Tidewater
Chesapeake, Virginia, 23320, United States
Emeritas Group Research
Lansdowne Town Center, Virginia, 20176, United States
Gastroenterology Consultants of Southwest Virginia
Roanoke, Virginia, 24014, United States
Sunshine Coast University Hospital
Birtinya, Queensland, 4575, Australia
Mater Adult Hospital
South Brisbane, Queensland, 4101, Australia
Princess Alexandra Hospital
Woolloongabba, Queensland, 4102, Australia
Royal Adelaide Hospital
Adelaide, South Australia, 5000, Australia
Queen Elizabeth Hospital
Woodville, South Australia, 5011, Australia
Northern Health
Epping, Victoria, 3076, Australia
Fiona Stanley Hospital
Murdoch, Western Australia, 6150, Australia
Medical University of Innsbruck
Innsbruck, 6020, Austria
University of Salzburg, Universitätsklinik für Innere Medizin III
Salzburg, 5020, Austria
Universitätsklinikum St. Pölten
Sankt Pölten, 3100, Austria
Medical University Vienna, Department of Internal Medicine III, Division Gastroenterology and Hepatology
Vienna, 1090, Austria
Universitaire Ziekenhuis Leuven
Leuven, 3000, Belgium
London Health Sciences Centre-University Hospital
London, N6A 5A5, Canada
Mount Sinai Hospital
Toronto, MSG 1X5, Canada
TDDA Speciality Research
Vaughan, L4L 4Y7, Canada
Centre Hospitalier Universitaire Grenoble
Grenoble, 38043, France
Hôpital Claude Huriez
Little Cedex, 59037, France
Hopital Saint Eloi
Montpellier, 34295, France
Centre Hospitalier Universitaire de Nantes
Nantes, 44000, France
Institut des MICI
Neuilly-sur-Seine, 92200, France
CHU de Saint Etienne - Hopital Nord
Saint-Etienne, 42055, France
Hopital Rangueil
Toulouse, 31059, France
CHRU Nancy
Vandœuvre-lès-Nancy, 54500, France
Charite Universitaetsmedizin Berlin Campus CVK, Department of Hepatology and Gastroenterology
Berlin, 13353, Germany
Medizinische Hochschule Hannover
Hanover, 30625, Germany
Universitatsklinikum Schleswig-Holstein
Kiel, 24105, Germany
Eugastro Gmbh
Liepzig, 4103, Germany
Universitaetsklinikum Ulm Klinik fur Innere Medizin I CED Studien Ambulanz
Ulm, 89081, Germany
Tolna Megye Balassa Janos Korhaz
Beri Balogh, 7100, Hungary
Szent Janos Korhaz es Eszak-budai Egyesitett Korhazak
Budapest, 1033, Hungary
AZIENDA UNICA OSPEDALIERO-UNIVERSITARIA"RENATO DULBECCO" - AOU"Mater Domini"
Catanzaro, 88100, Italy
IRCCS Istituto Clinico Humanitas
Milan, 20089, Italy
Azienda Ospedaliera San Camillo Forlanini
Roma, 00152, Italy
Istituto Clinico Humanitas
Rozzano, 20089, Italy
Hyogo Medical University Hospital
Hyōgo, 663-8501, Japan
Fukuoka University Hospital
Jonan-ku, 814-0180, Japan
The Jikei University Hospital
Minatoku, 105-8471, Japan
Kitasato University Kitasato Institute Hospital
Minatoku, 108-8642, Japan
Kyorin University Hospital
Mitaka-shi, 181-8611, Japan
Nagasaki University Hospital
Nagasaki, 852-8501, Japan
Ishida Clinic of IBD and Gastroenterology
Ōita, 870-0823, Japan
Saga University Hospital
Sagaken, 849-8501, Japan
Kitasato University Hospital
Sagamihara, 252-0375, Japan
Sapporo Medical University Hospital
Sapporo, 060-8543, Japan
Ginza Central Clinic
Tokyo, 104-0061, Japan
Institute of Science Tokyo Hospital
Toukiyouto, 113-8519, Japan
Gabinet Endoskopii Przewodu Pokarmowego
Krakow, 31-009, Poland
Medrise Sp. z o.o. Centrum Badań Klinicznych
Lublin, 20-852, Poland
SOLUMED Centrum Medyczne
Poznan, 60-425, Poland
Kliniczny Szpital Wojewódzki Nr 2 im. Sw. Jadwigi Królowej w Rzeszowie
Rzeszów, 35-210, Poland
Specjalistyczna Praktyka Lekarska Leszek Bryniarski
Sopot, 81-756, Poland
Medical Network Sp. z o.o. WIP Warsaw IBD Point Profesor Kierkus
Warsaw, 00-728, Poland
Specjalistyczne Gabinety Lekarskie Body Clinic
Warsaw, 03-712, Poland
Centrum Medyczne Oporow
Wroclaw, 52-416, Poland
Yonsei University Severance Hospital
Seodaemun-Gu, VIC, 3772, South Korea
Inje University
Busan, 48108, South Korea
Yeungnam University Hospital
Daegu, 42415, South Korea
Kyungpook National University Hospital
Junggu, 41944, South Korea
Kangbuk Samsung Hospital
Seoul, 03181, South Korea
Hanyang University Hospital
Seoul, 04763, South Korea
Samsung Medical Center
Seoul, 06351, South Korea
Intesto, Gastroenterologische Praxis Crohn-Colitis-Zentrum
Bern, 3012, Switzerland
Fairfield General Hospital
Bury, BL9 7TD, United Kingdom
Cambridge University Hospitals NHS Foundation Trust
Cambridge, CB2 0QQ, United Kingdom
Barts Health NHS Trust
London, E1 2AJ, United Kingdom
Norfolk and Norwich University Hospital Nhs Foundation Trust
Norwich, NR4 7UZ, United Kingdom
University Hospital Southampton Nhs Foundation Trust
Southampton, SO16 6YD, United Kingdom
Related Publications (1)
Madia PA, Wendt ER, Qin AR, Qi X, Liang Y, Kalariya S, Hong F, Canales E, Taylor JG, Arulmani U, Kakkar T. First-In-Human Evaluation of the Pharmacokinetics, Pharmacodynamics, and Safety of Tilpisertib Fosmecarbil (GS-5290), an Oral Prodrug of a Tumor Progression Locus 2 Inhibitor in Healthy Participants. J Clin Pharmacol. 2026 Aug;66(8):e70269. doi: 10.1002/jcph.70269.
PMID: 42634341DERIVED
Related Links
MeSH Terms
Conditions
Condition Hierarchy (Ancestors)
Study Officials
- STUDY DIRECTOR
Gilead Study Director
Gilead Sciences
Study Design
- Study Type
- interventional
- Phase
- phase 2
- Allocation
- RANDOMIZED
- Masking
- DOUBLE
- Who Masked
- PARTICIPANT, INVESTIGATOR
- Purpose
- TREATMENT
- Intervention Model
- PARALLEL
- Sponsor Type
- INDUSTRY
- Responsible Party
- SPONSOR
Study Record Dates
First Submitted
September 1, 2023
First Posted
September 8, 2023
Study Start
December 5, 2023
Primary Completion (Estimated)
January 1, 2027
Study Completion (Estimated)
February 1, 2028
Last Updated
September 11, 2026
Record last verified: 2026-09
Data Sharing
- IPD Sharing
- Will not share