NCT03010982

Open-Label, Multi-Center, Two-Part, Ph1 Study to Characterize the PKs of an Intravenous Micro-Dose of [14C]-Tazemetostat (EPZ 6438) and the ADME of an Oral [14C]-Labeled Dose of Tazemetostat in Subjects With B-Cell Lymphomas or Adv Solid Tumors

Completed Phase 1 Last updated 22 March 2024

What this trial tests

Phase 1 trial testing Tazemetostat and [14C] Tazemetostat in Diffuse Large B Cell Lymphoma in 3 participants. Completed in 8 January 2019.

Timeline

20 June 2018

Primary endpoint
8 January 2019

8 January 2019

Quick facts

Lead sponsor	Epizyme, Inc.
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	na
Design	single group
Masking	none
Primary purpose	treatment
Enrollment	3
Start date	20 June 2018
Primary completion	8 January 2019
Estimated completion	8 January 2019
Sites	2 locations across United Kingdom

Drugs / interventions tested

• Tazemetostat and [14C] Tazemetostat — full drug profile →

Conditions studied

• Diffuse Large B Cell Lymphoma — all drugs for Diffuse Large B Cell Lymphoma →
• Primary Mediastinal Lymphoma — all drugs for Primary Mediastinal Lymphoma →
• Mantle-Cell Lymphoma — all drugs for Mantle-Cell Lymphoma →
• Follicular Lymphoma — all drugs for Follicular Lymphoma →

Sponsor

Epizyme, Inc. — full company profile →

Who can join

18 and older, any sex, with Diffuse Large B Cell Lymphoma or Primary Mediastinal Lymphoma. Patients with the condition only — healthy volunteers not accepted.

Sponsor's own description

This is a Phase 1, open-label, two-part study designed to characterize the PK of an IV dose of approximately 12 µg tazemetostat that contains approximately 500 nCi of \[14C\] tazemetostat and the ADME of an oral dose of 800 mg tazemetostat that contains approximately 400 µCi of \[14C\]-labeled tazemetostat in three subjects with B-cell lymphomas or advanced solid tumors.

Publications & conference data

8 peer-reviewed publications reference this trial (live from Europe PMC):

1. EZH2-Targeted Therapies in Cancer: Hype or a Reality.
   Eich ML, Athar M, Ferguson JE, Varambally S. · · 2020 · cited 188× · PMID 32978169 · DOI 10.1158/0008-5472.can-20-2147
2. Androgen deprivation promotes neuroendocrine differentiation and angiogenesis through CREB-EZH2-TSP1 pathway in prostate cancers.
   Zhang Y, Zheng D, Zhou T, Song H, et al · · 2018 · cited 171× · PMID 30287808 · DOI 10.1038/s41467-018-06177-2
3. The role of histone methylation in the development of digestive cancers: a potential direction for cancer management.
   Chen Y, Ren B, Yang J, Wang H, et al · · 2020 · cited 102× · PMID 32747629 · DOI 10.1038/s41392-020-00252-1
4. The roles of EZH2 in cancer and its inhibitors.
   Liu Y, Yang Q. · · 2023 · cited 100× · PMID 37148376 · DOI 10.1007/s12032-023-02025-6
5. Emerging epigenetic-modulating therapies in lymphoma.
   Sermer D, Pasqualucci L, Wendel HG, Melnick A, et al · · 2019 · cited 97× · PMID 30837715 · DOI 10.1038/s41571-019-0190-8
6. EZH2 abnormalities in lymphoid malignancies: underlying mechanisms and therapeutic implications.
   Li B, Chng WJ. · · 2019 · cited 71× · PMID 31752930 · DOI 10.1186/s13045-019-0814-6
7. Polycomb complexes in normal and malignant hematopoiesis.
   Di Carlo V, Mocavini I, Di Croce L. · · 2019 · cited 48× · PMID 30341152 · DOI 10.1083/jcb.201808028
8. EZH2 as a therapeutic target for multiple myeloma and other haematological malignancies.
   Tremblay-LeMay R, Rastgoo N, Pourabdollah M, Chang H. · · 2018 · cited 46× · PMID 30555699 · DOI 10.1186/s40364-018-0148-5