Tolinapant

Generic Name: Tolinapant

Drug Type: Small Molecule

Chemical Formula: C_₃₀H_₄₂FN_₅O_₃

CAS Number: 1799328-86-1

Unique Ingredient Identifier: 2LHZ9ZC3YO

Background: ASTX660 is under investigation in clinical trial NCT02503423 (Phase 1-2 Study of ASTX660 in Subjects With Advanced Solid Tumors and Lymphomas).

Clinical Trials

Testing the Addition of an Investigational Anti-Cancer Drug, ASTX660 (Tolinapant), to a Usual Chemotherapy Treatment (Eribulin) for Treatment of Advanced Triple Negative Breast Cancer

Phase 1

Suspended

Conditions: Anatomic Stage III Breast Cancer AJCC v8
Anatomic Stage IV Breast Cancer AJCC v8
Invasive Breast Carcinoma
Locally Advanced HER2-Negative Breast Carcinoma
Locally Advanced Hormone Receptor-Positive Breast Carcinoma
Locally Advanced Triple-Negative Breast Carcinoma
Metastatic HER2-Negative Breast Carcinoma
Metastatic Hormone Receptor-Positive Breast Carcinoma
Metastatic Triple-Negative Breast Carcinoma
Unresectable HER2-Negative Breast Carcinoma

Interventions: Procedure: Biopsy Procedure
Procedure: Biospecimen Collection
Procedure: Computed Tomography
Drug: Eribulin Mesylate
Procedure: Magnetic Resonance Imaging
Drug: Tolinapant
Procedure: X-Ray Imaging

First Posted Date: 2024-09-19

Last Posted Date: 2025-04-22

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 42

Registration Number: NCT06590558

Locations: 🇺🇸
University of Kentucky/Markey Cancer Center, Lexington, Kentucky, United States
🇺🇸
Ohio State University Comprehensive Cancer Center LAO, Columbus, Ohio, United States
🇺🇸
Huntsman Cancer Institute/University of Utah, Salt Lake City, Utah, United States

Testing the Addition of ASTX660 (Tolinapant) to the Usual Chemotherapy Treatment (Paclitaxel With or Without Bevacizumab) in Patients With Recurrent Ovarian Cancer

Phase 1

Not yet recruiting

Conditions: Recurrent Fallopian Tube High Grade Serous Adenocarcinoma
Recurrent High Grade Endometrioid Adenocarcinoma
Recurrent Ovarian Seromucinous Carcinoma
Recurrent Ovarian Undifferentiated Carcinoma
Recurrent Platinum-Resistant Ovarian Carcinoma
Platinum-Refractory Fallopian Tube Carcinoma
Platinum-Refractory Primary Peritoneal Carcinoma
Recurrent Fallopian Tube Carcinosarcoma
Platinum-Refractory Ovarian Carcinoma
Recurrent Fallopian Tube Undifferentiated Carcinoma

Interventions: Biological: Bevacizumab
Procedure: Biospecimen Collection
Procedure: Computed Tomography
Procedure: Magnetic Resonance Imaging
Drug: Paclitaxel
Drug: Tolinapant

First Posted Date: 2024-05-01

Last Posted Date: 2025-05-08

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 127

Registration Number: NCT06393751

Preoperative Radiotherapy And ASTX660 in Rectum Cancer

Phase 1

Recruiting

Conditions: Locally-advanced Rectal Cancer

Interventions: Drug: TOLINAPANT (ASTX660)
Drug: mFOLFIRINOX
Radiation: Pelvic radiotherapy LCRT
Radiation: Pelvic radiotherapy SCRT
Drug: FOLFOX4
Drug: Capecitabine
Drug: CAPOX

First Posted Date: 2023-06-22

Last Posted Date: 2024-02-08

Lead Sponsor: Gustave Roussy, Cancer Campus, Grand Paris

Target Recruit Count: 78

Registration Number: NCT05912075

Locations: 🇫🇷
Centre Léon Bérard, Lyon, Rhöne, France
🇫🇷
Gustave Roussy, Villejuif, Val De Marne, France

A Study of Tolinapant in Combination With Oral Decitabine/Cedazuridine and Oral Decitabine/Cedazuridine Alone in Participants With Relapsed/Refractory Peripheral T-cell Lymphoma (R/R PTCL)

Phase 1

Active, not recruiting

Conditions: Relapsed/Refractory Peripheral T-cell Lymphoma

Interventions: Drug: Tolinapant
Drug: Decitabine + Cedazuridine

First Posted Date: 2022-06-03

Last Posted Date: 2025-05-02

Lead Sponsor: Taiho Oncology, Inc.

Target Recruit Count: 33

Registration Number: NCT05403450

Locations: 🇫🇷
Institut Gustave Roussy, Villejuif, France
🇫🇷
Institut Paoli-Calmettes, Marseille, France
🇦🇺
Concord Hospital, Concord, New South Wales, Australia

and more 43 locations

Tolinapant and Radiation for Cisplatin-Ineligible, Previously Untreated, Locally Advanced Head and Neck Cancer

Early Phase 1

Active, not recruiting

Conditions: Locally Advanced Laryngeal Squamous Cell Carcinoma
Head and Neck Carcinoma of Unknown Primary
Locally Advanced Head and Neck Squamous Cell Carcinoma
Locally Advanced Oropharyngeal Squamous Cell Carcinoma
Locally Advanced Hypopharyngeal Squamous Cell Carcinoma
Locally Advanced Nasopharyngeal Squamous Cell Carcinoma

Interventions: Drug: Tolinapant
Radiation: Radiation Therapy

First Posted Date: 2022-02-18

Last Posted Date: 2025-03-17

Lead Sponsor: Emory University

Target Recruit Count: 10

Registration Number: NCT05245682

Locations: 🇺🇸
Emory University/Winship Cancer Institute, Atlanta, Georgia, United States

ASTEROID: A Trial of ASTX660 in Combination With Pembrolizumab

Phase 1

Recruiting

Conditions: Advanced Cancer
Cervical Cancer
Triple Negative Breast Cancer

Interventions: Drug: ASTX660
Drug: Pembrolizumab

First Posted Date: 2021-10-18

Last Posted Date: 2025-05-20

Lead Sponsor: Institute of Cancer Research, United Kingdom

Target Recruit Count: 48

Registration Number: NCT05082259

Locations: 🇬🇧
Cambridge University Hospitals NHS Trust, Cambridge, United Kingdom
🇬🇧
The Royal Marden NHS Foundation Trust - Drug Development Unit, Sutton, United Kingdom
🇬🇧
The Royal Marsden NHS Foundation Trust - Breast Unit, Sutton, United Kingdom

Effect of Food on the Pharmacokinetics of ASTX660 in Healthy Volunteers

Phase 1

Completed

Conditions: Healthy Volunteer

Interventions: Drug: ASTX660

First Posted Date: 2020-07-21

Last Posted Date: 2024-08-02

Lead Sponsor: Astex Pharmaceuticals, Inc.

Target Recruit Count: 21

Registration Number: NCT04479800

Locations: 🇺🇸
Worldwide Clinical Trials, San Antonio, Texas, United States

A Study to Investigate the Effect of CYP3A4 Inhibition on the Single Dose Pharmacokinetics of ASTX660 and the Effect of a Single Dose of ASTX660 on the Pharmacokinetics of the CYP3A4 Substrate Midazolam

Phase 1

Completed

Conditions: Healthy Volunteer

Interventions: Drug: ASTX660
Drug: Midazolam
Drug: Itraconazole

First Posted Date: 2020-06-01

Last Posted Date: 2024-08-02

Lead Sponsor: Astex Pharmaceuticals, Inc.

Target Recruit Count: 36

Registration Number: NCT04411030

Locations: 🇺🇸
QPS Bio-kinetic, Springfield, Missouri, United States

A Phase I/II Study of ASTX660 in Patients With Relapsed or Refractory T-cell Lymphoma

Phase 1

Terminated

Conditions: Relapsed or Refractory Peripheral T-cell Lymphoma(PTCL),Cutaneous T-cell Lymphoma(CTCL),Adult T-cell Leukemia/Lymphoma(ATLL)

Interventions: Drug: ASTX660

First Posted Date: 2020-04-24

Last Posted Date: 2025-01-15

Lead Sponsor: Otsuka Pharmaceutical Co., Ltd.

Target Recruit Count: 61

Registration Number: NCT04362007

Locations: 🇯🇵
Yamagata University Hospital, Yamagata, Japan

A Study of ASTX660 as a Single Agent and in Combination With ASTX727 in Subjects With Relapsed/Refractory Acute Myeloid Leukemia (AML)

Phase 1

Terminated

Conditions: Acute Myeloid Leukemia

Interventions: Drug: ASTX660
Drug: ASTX727

First Posted Date: 2019-11-07

Last Posted Date: 2024-08-02

Lead Sponsor: Astex Pharmaceuticals, Inc.

Target Recruit Count: 68

Registration Number: NCT04155580

Locations: 🇺🇸
The University of Chicago Medical Center, Chicago, Illinois, United States
🇺🇸
Franciscan Health Indianapolis (Blood and Marrow Transplantation), Indianapolis, Indiana, United States
🇺🇸
Ohio State University Comprehensive Cancer Center, Columbus, Ohio, United States

and more 12 locations

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