A Phase Ib/II, Dose Escalation and Dose Expansion Study of Valemetostat Tosylate (DS-3201b) With Atezolizumab and Bevacizumab in Advanced Hepatocellular Carcinoma (HCC)

This is a phase Ib/II, dose escalation and dose expansion study of valemetostat (DS-3201) with atezolizumab and bevacizumab in patients advanced Hepatocellular carcinoma (HCC) who did not receive prior systemic therapy for advanced HCC.

Start Date31 Oct 2024

Sponsor / Collaborator

The University of Alabama at Birmingham

NCT05879484 / Not yet recruitingPhase 1/2IIT

A Phase Ib/II Multicenter Study of Front Line Pembrolizumab and Valemetostat in PD-L1 Positive, HPV-Negative Recurrent/Metastatic Squamous Cell Carcinoma (SCC) of the Head and Neck: The PANTHERAS

Background:
Head and neck squamous cell carcinoma (HNSCC) is the 6th most common cancer worldwide. These cancers have different causes, with smoking/tobacco exposure and human papilloma virus infection being the most common. . When HNSCC occurs in people who are not infected with HPV, the cancers are more likely to return after treatment; when this happens, overall survival is only about 10 months, thus better treatments are needed.
Objective:
To test a combination treatment using 2 drugs (valemetostat and pembrolizumab) in people with HNSCC. Phase 1b of the study will determine a recommended dose of the 2 drugs and evaluate how safe the combination is.; this will include patients with HPV-positive and HPV-negative HNSCC, as well as squamous cell NSCLC that have progressed on anti-PD-1/anti-PD-L1 therapies.Phase II will determine how effective the combination is and will focus on patients with HPV-negative HNSCC.
Eligibility:
People aged 18 years and older with HPV-negative HNSCC, sinonasal carcinoma of the head and neck, or squamous non-small cell lung cancer (NSCLC).
Design:
Participants will be screened. They will have a physical exam. They will have blood and urine tests and tests of their heart function. They will have imaging scans. They may have a biopsy: A small sample of tissue will be removed from the tumor.
Treatment will be given in 21-day cycles.
Pembrolizumab is administered through a tube attached to a needle inserted into a vein in the arm. Participants will receive pembrolizumab on the first day of each cycle.
Valemetostat is a tablet taken by mouth. Participants will take the tablet once a day at home. They will record the date and time of each dose in a diary. They will also write down any adverse effects they experience.
Participants may remain in the study up to 2 years.

Start Date27 Jun 2024

Sponsor / Collaborator

National Cancer Institute

NCT06244485 / RecruitingPhase 1

A Phase 1b, Multicenter, Open-Label Study of Valemetostat Tosylate in Combination With DXd ADCs in Subjects With Solid Tumors

This study will evaluate the safety, tolerability, and efficacy of valemetostat tosylate in combination with DXd ADC in patients with advanced solid tumors.

Start Date16 Feb 2024

Sponsor / Collaborator

Daiichi Sankyo Co., Ltd.

100 Clinical Results associated with Valemetostat Tosilate

100 Translational Medicine associated with Valemetostat Tosilate

100 Patents (Medical) associated with Valemetostat Tosilate

Literatures (Medical) associated with Valemetostat Tosilate

01 Jan 2024·Clinical pharmacology in drug development

Safety, Tolerability, and Pharmacokinetics of Valemetostat Tablets and the Effect of Food on Valemetostat Pharmacokinetics in Healthy Subjects: Two Phase 1 Studies

Article

Author: Shimizu, Takako ; Ishizuka, Hitoshi ; Tsutsumi, Junko ; Tachibana, Masaya ; Toyama, Kaoru ; Maekawa, Yutaro ; Fukae, Masato ; Shinohara, Sayaka ; Matsuki, Shunji

Abstract:

Valemetostat is an oral, selective inhibitor of enhancer of zeste homolog‐2 (EZH2) and EZH1. In a first‐in‐human phase‐1 trial, valemetostat capsules were well tolerated and clinically active in patients with relapsed/refractory non‐Hodgkin lymphoma. Subsequently, a film‐coated tablet formulation was developed for future clinical trials and commercialization. We report outcomes from 2 phase 1 trials in healthy Japanese participants, assessing the safety, tolerability, and pharmacokinetics (PK) of valemetostat tablets at single ascending doses (50, 100, and 200‐mg), the relative bioavailability between capsules and tablets, and the effect of food (high‐fat or low‐fat meals) on the PK of valemetostat tablets. In the ascending‐dose study, valemetostat maximum plasma concentration (Cmax) and area under the concentration–time curve (AUC) increased dose‐proportionally. Valemetostat plasma PK parameters were similar between the capsule and tablet formulations following a single 200‐mg dose. Administration of valemetostat, 200 mg after a meal, was associated with 50%‐60% lower Cmax, 30%‐50% lower AUC, and a median Tmax delay of 2.5‐3 hours relative to fasted administration. Valemetostat was well tolerated in healthy subjects; treatment‐emergent adverse events were mild (grade 1) in severity. Based on these trials, the tablet formulation of valemetostat is suitable for use in subsequent clinical trials and should be administered under fasted conditions to avoid a negative food effect.

07 Dec 2023·Japanese journal of clinical oncology

An update on the developments in the treatment of adult T-cell leukemia–lymphoma: current knowledge and future perspective

Review

Author: Makiyama, Junya ; Ishitsuka, Kenji ; Maruyama, Dai ; Nagai, Hirokazu ; Munakata, Wataru

Abstract:

Adult T-cell leukemia–lymphoma is defined as peripheral T-cell lymphoma caused by the human T-cell leukemia virus type I. Adult T-cell leukemia–lymphoma is classified into indolent (favorable chronic or smoldering) or aggressive (acute, lymphoma or unfavorable chronic) types. This review discusses the therapeutic developments for patients with adult T-cell leukemia–lymphoma and unmet issues in treating adult T-cell leukemia–lymphoma. For indolent adult T-cell leukemia–lymphoma, a watchful waiting strategy is recommended until the disease progresses to aggressive adult T-cell leukemia–lymphoma. For aggressive adult T-cell leukemia–lymphoma, multi-agent chemotherapy with or without allogeneic hematopoietic stem cell transplantation has been recommended. However, many patients with adult T-cell leukemia–lymphoma relapse, and their prognosis is poor. Recently, novel agents, including mogamulizumab, lenalidomide, brentuximab vedotin, tucidinostat and valemetostat, have been approved for patients with relapsed or refractory aggressive adult T-cell leukemia–lymphoma, and the combination of mogamulizumab with multi-agent chemotherapy or brentuximab vedotin with cyclophosphamide, doxorubicin and prednisone has been approved for patients with untreated aggressive adult T-cell leukemia–lymphoma in Japan. Importantly, the aging of patients with adult T-cell leukemia–lymphoma has recently been reported, and no standard of care for elderly patients with adult T-cell leukemia–lymphoma has been established. New evidence must be obtained from prospective clinical trials to improve the prognosis of patients with adult T-cell leukemia–lymphoma.

01 Nov 2023·Clinical and translational science

Effect of itraconazole and fluconazole on the pharmacokinetics of valemetostat: An open‐label, phase I study in healthy subjects

Article

Author: Tsutsumi, Junko ; Ishizuka, Hitoshi ; Shimizu, Takako ; Tachibana, Masaya ; Maekawa, Yutaro ; Matsuki, Shunji ; Kuroda, Kana

Abstract:

Valemetostat tosylate (valemetostat) is an oral, potent, dual inhibitor of enhancer of zeste homolog (EZH) 2 and EZH1 under investigation for the treatment of cancer, including non‐Hodgkin's lymphomas and solid tumors. Itraconazole and fluconazole are antifungal medications often used as typical inhibitors of cytochrome P450 3A (CYP3A [itraconazole and fluconazole]) and P‐glycoprotein (P‐gp [itraconazole]) in drug–drug interaction studies. Valemetostat is a substrate of CYP3A and P‐gp in vitro. This phase I, open‐label, single‐sequence crossover study (JapicCTI‐183902) assessed the pharmacokinetics (PK) of valemetostat when co‐administered with itraconazole (a strong CYP3A inhibitor and P‐gp inhibitor) or fluconazole (a moderate CYP3A inhibitor) in healthy Japanese male participants 20–45 years of age. Participants were equally allocated to receive two doses of valemetostat 25 mg, once alone and once with either itraconazole or fluconazole (400‐mg induction and 200‐mg once daily maintenance). Valemetostat PK parameters with versus without itraconazole or fluconazole were compared using analysis of variance models. Overall, 32 participants were enrolled. Co‐administration with itraconazole increased valemetostat peak concentration (Cmax) by 2.9‐fold and area under the plasma concentration–time curve extrapolated to infinity (AUCinf) by 4.2‐fold compared with valemetostat alone. When co‐administered with fluconazole, the Cmax and AUCinf of valemetostat were each increased by 1.6‐fold. No treatment‐related or grade ≥3 adverse events were reported. Appropriate valemetostat dose reductions are warranted when used concomitantly with strong CYP3A and P‐gp dual inhibitors.

News (Medical) associated with Valemetostat Tosilate

25 Jun 2024

·pipelinereview.com

EZHARMIA® Approved in Japan as First Dual EZH1 and EZH2 Inhibitor Therapy for Patients with Peripheral T-Cell Lymphoma

TOKYO, Japan I June 24, 2024 I Daiichi Sankyo’s (TSE: 4568) EZHARMIA® (valemetostat tosilate) has been approved in Japan for the treatment of adult patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). EZHARMIA is now the first dual inhibitor of EZH1 and EZH2 to be approved for PTCL after receiving SAKIGAKE designation for this indication. PTCL is a group of rare and often aggressive blood cancers, which represent about 10 to 15% of all non-Hodgkin lymphomas (NHL).1 PTCL is more common in Asia, including in Japan, compared to other parts of the world.2 A majority of patients with PTCL experience disease progression following initial treatment with a multi-drug chemotherapy-based regimen and median overall survival following relapse is approximately 5.8 months.1 The approval of EZHARMIA by the Japan Ministry of Health, Labour and Welfare (MHLW) is based on results of the VALENTINE-PTCL01 phase 2 trial, which were presented at the 2023 American Society of Hematology (ASH) Annual Meeting. In VALENTINE-PTCL01, an objective response rate (ORR) of 43.7% (n=52, 95% CI: 34.6-53.1) was observed for EZHARMIA in 119 efficacy evaluable patients with relapsed or refractory PTCL as assessed by CT-based blinded independent central review (BICR). Seventeen complete responses (CRs) and 35 partial responses (PRs) were observed. Responses were seen across a variety of PTCL subtypes including angioimmunoblastic T-cell lymphoma (AITL), PTCL not otherwise specified (PTCL-NOS) and other PTCL subtypes. “This second indication for EZHARMIA in Japan is an important advance for the treatment of relapsed or refractory peripheral T-cell lymphoma, as new and effective treatment options are needed to improve patient outcomes,” said Toshinori Agatsuma, PhD, Executive Officer, Head of R&D Division in Japan, Daiichi Sankyo. “EZHARMIA exemplifies the innovative research being conducted by Daiichi Sankyo aimed at creating new medicines with potential to change the standard of care for patients with cancer.” The safety profile of EZHARMIA in VALENTINE-PTCL01 was consistent with previous clinical trials. Treatment-related adverse events occurred in 106 of 133 patients (79.7%) with the most common including platelet count decrease (44.4%), anemia (27.1%), dysgeusia (24.8%) and neutrophil count decrease (21.1%). About VALENTINE-PTCL01 Trial VALENTINE-PTCL01 is a global, open-label, single-arm, two-cohort phase 2 study evaluating the efficacy and safety of EZHARMIA in patients with relapsed or refractory PTCL and adult T-cell leukemia/lymphoma (ATLL) who received at least one systemic therapy and were ineligible for hematopoietic stem cell transplant at the time of screening. One cohort enrolled patients with PTCL and a second cohort enrolled patients with ATLL. The primary endpoint of VALENTINE-PTCL01 is ORR assessed by CT-based BICR. Secondary endpoints include duration of response, CR, PR, duration of CR and progression-free survival – all assessed by both BICR and investigator assessment – as well as ORR assessed by investigator, overall survival, safety and pharmacokinetics. Exploratory endpoints include PET-CT-based BICR and biomarker mutational status. Responses were evaluated based on Lugano 2014 response criteria. VALENTINE-PTCL01 enrolled 133 patients at multiple sites in Asia, Europe, North America and Oceania. For more information about this study, visit ClinicalTrials.gov. About Peripheral T-Cell Lymphoma PTCL is a group of rare and often aggressive blood cancers, which represent 10 to 15% of all NHLs.1 Approximately 553,000 new cases of NHL were diagnosed worldwide in 2022.3 There are at least 29 recognized subtypes of PTCL, which occur with significant geographic variation.4 PTCL is more common in Asia, including in Japan, compared to other parts of the world.2 Prognosis of PTCL is generally poor, with a five-year overall survival rate of 32% in AITL and PTCL-NOS, and 7% or lower in certain subtypes.5 A majority of patients with PTCL experience disease progression following initial treatment with a multi-drug chemotherapy-based regimen and median overall survival following relapse is approximately 5.8 months.1 Development of more effective medicines for PTCL continues to be an unmet clinical need, particularly in the relapsed or refractory setting.1 About EZH1 and EZH2 The EZH1 (enhancer of zeste homolog 1) and EZH2 (enhancer of zeste homolog 2) enzymes help regulate the expression of genes involved in maintaining healthy hematopoietic stem cells (immature blood cells).6 Both enzymes are recurrently mutated or overexpressed in hematologic malignancies, including T-cell lymphomas, and research shows they contribute to the silencing of tumor suppressor genes and drive oncogenic growth. 7,8 About EZHARMIA EZHARMIA (valemetostat tosilate) is first-in-class dual inhibitor of EZH1 and EZH2 that was discovered by Daiichi Sankyo. EZHARMIA is approved in Japan for the treatment of patients with relapsed or refractory PTCL and for the treatment of patients with relapsed or refractory ATLL. It is an investigational medicine in all countries outside of Japan. About EZHARMIA Clinical Development Program A global clinical development program is underway for EZHARMIA in hematologic and solid cancers. In addition to VALENTINE-PTCL01, EZHARMIA is being evaluated in the VALYM phase 2 trial in patients with relapsed or refractory B-cell lymphomas, which is being conducted under a strategic research collaboration with the LYSA-LYSARC-CALYM group in Europe, and a phase 1b study in combination with DXd antibody drug conjugates ENHERTU® (trastuzumab deruxtecan) and datopotamab deruxtecan (Dato-DXd) in patients with solid cancers. About Daiichi Sankyo Daiichi Sankyo is an innovative global healthcare company contributing to the sustainable development of society that discovers, develops and delivers new standards of care to enrich the quality of life around the world. With more than 120 years of experience, Daiichi Sankyo leverages its world-class science and technology to create new modalities and innovative medicines for people with cancer, cardiovascular and other diseases with high unmet medical need. For more information, please visit www.daiichisankyo.com . References 1 Bellei et al. haematologica. Vol. 103 No. 7 (2018): July 2018 2 Vose JM et al. J Clin Oncol. 2008;26:4124-4130 3 Global Cancer Observatory. Cancer Fact Sheet. February 2024 4 Liang X et al. Medicine 2021; 2021 Apr 2;100(13): e25194. 5 Vose JM et al. J Clin Oncol. 2008;26:4124-4130 6 Honma D et al. Cancer Sci. 2017 Oct; 108(10): 2069–2078 7 Nakagawa M and Kitabayashi I. Cancer Sci. 2018;109:2342–2348 8 Yamagishi et al. Cell Reports. 2019; 29, 2321–2337

Phase 2Clinical ResultDrug ApprovalASHPhase 1

24 Jun 2024

·www.pharmaceutical-technology.com

Daiichi Sankyo peripheral T-cell lymphoma therapy approved in Japan

The asset previously received SAKIGAKE designation in Japan. Credit: Nemes Laszlo / Shutterstock. Daiichi Sankyo has announced approval from the Japan Ministry of Health, Labour and Welfare for EZHARMIA (valemetostat tosilate) to treat relapsed or refractory (r/r) peripheral T-cell lymphoma (PTCL). EZHARMIA is the first dual EZH1 and EZH2 inhibitor to receive approval for this indication. The asset previously received the SAKIGAKE designation. Its approval is grounded in the outcomes of the global, open-label, single-arm, two-cohort VALENTINE-PTCL01 Phase II trial. The trial assessed the efficacy and safety of EZHARMIA in patients with relapsed or refractory PTCL and adult T-cell leukemia/lymphoma who had previously undergone at least one systemic therapy and were ineligible for a hematopoietic stem cell transplant at screening. See Also: Johnson & Johnson seeks FDA approval for Tremfya for Crohn’s disease AstraZeneca’s Truqap and Faslodex combo receives approval in EU It enrolled 133 patients across multiple sites in Europe, Asia, North America and Oceania, The primary endpoint of the trial was objective response rate (ORR) with secondary endpoints being the duration of response, complete response (CR), partial response (PR), duration of CR, progression-free survival, overall survival, safety and pharmacokinetics. In the study, EZHARMIA demonstrated an ORR of 43.7% in 119 efficacy-evaluable patients with relapsed or refractory PTCL. The treatment also led to 17 CRs and 35 PRs, with responses observed across various PTCL subtypes, including angioimmunoblastic T-cell lymphoma, PTCL not otherwise specified and other PTCL subtypes. Daiichi Sankyo Japan research and development division head and executive officer Toshinori Agatsuma stated: “This second indication for EZHARMIA in Japan is an important advance for the treatment of relapsed or refractory peripheral T-cell lymphoma, as new and effective treatment options are needed to improve patient outcomes. EZHARMIA exemplifies the innovative research being conducted by Daiichi Sankyo aimed at creating new medicines with the potential to change the standard of care for patients with cancer.”

Clinical ResultDrug ApprovalPhase 2Cell TherapyImmunotherapy

21 May 2024

·www.biospace.com

Daiichi Sankyo Highlights Progress in Creating New Standards of Care for Patients Across Multiple Cancers at ASCO

ENHERTU® late-breaking data from DESTINY-Breast06 continues to redefine the classification and treatment of metastatic breast cancer with new data in patients with HER2 low and HER2 ultralow disease Updated survival results from DESTINY-Breast03 trial of ENHERTU in patients with previously treated HER2 positive metastatic breast cancer also to be presented Investor meeting to discuss ASCO presentations and oncology development updates BASKING RIDGE, N.J.--(BUSINESS WIRE)--Daiichi Sankyo (TSE: 4568) will present new clinical research across its oncology portfolio with more than 45 abstracts in multiple cancers at the 2024 American Society of Clinical Oncology Scientific Program (#ASCO24). Data at ASCO showcasing the company’s progress in creating new standards of care for patients with cancer will include the late-breaking positive results of the DESTINY-Breast06 phase 3 trial (LBA #1000) evaluating ENHERTU® (trastuzumab deruxtecan) compared to standard of care chemotherapy in patients with HR positive, HER2 low (IHC 1+ or IHC 2+/ISH-) or HER2 ultralow [defined as IHC 0 with membrane staining; IHC >0 <1+] metastatic breast cancer following one or more lines of endocrine therapy. Data from DESTINY-Breast06 will be featured in an ASCO press briefing. “Results to be shared at ASCO from DESTINY-Breast06 demonstrate how ENHERTU continues to challenge the traditional classification and treatment of breast cancer, building on the practice-changing results seen with DESTINY-Breast04,” said Ken Takeshita, MD, Global Head, R&D, Daiichi Sankyo. “These significant data along with updated survival results from DESTINY-Breast03 highlight how ENHERTU is a transformative medicine for the treatment of certain patients with metastatic breast cancer.” Updated survival results from the DESTINY-Breast03 phase 3 trial (#1025) of ENHERTU versus trastuzumab emtansine (T-DM1) in patients with previously treated HER2 positive metastatic breast cancer along with interim results from the dose expansion portion of DESTINY-Breast07 phase 1b/2 trial (#1009) evaluating ENHERTU monotherapy as well as ENHERTU plus pertuzumab in patients with previously untreated HER2 positive metastatic breast cancer also will be presented. Additional ENHERTU data at ASCO includes the final results of the DESTINY-Lung02 phase 2 trial (#8543) in patients with previously treated HER2 mutant non-small cell lung cancer (NSCLC) as well as three sub-analyses from the DESTINY-PanTumor02 phase 2 trial in patients with HER2 expressing metastatic biliary tract and pancreatic cancer (#4090), bladder cancer (#4565) and head and neck cancer (#6037). Data from DESTINY-PanTumor02 was one of three phase 2 trials that led to the recent accelerated approval in the U.S. of ENHERTU for a tumor agnostic indication in unresectable or metastatic HER2 positive (IHC 3+) solid tumors. Additional Data and Trials-in-Progress Across Daiichi Sankyo’s DXd ADC Portfolio at ASCO Additional sub-analyses from the TROPION-Lung02 phase 1b trial (#8617) evaluating datopotamab deruxtecan (Dato-DXd) in combination with pembrolizumab with or without platinum chemotherapy as a first-line treatment for patients with advanced or metastatic NSCLC, the intracranial efficacy of datopotamab deruxtecan in patients with advanced or metastatic NSCLC with actionable genomic alterations from the TROPION-Lung05 phase 2 trial (#8593), and patient reported outcomes from the TROPION-Breast01 phase 3 trial (#1006) of datopotamab deruxtecan versus chemotherapy in patients with previously treated inoperable or metastatic hormone receptor positive, HER2 negative breast cancer will be presented. Trials-in-progress presentations include the IDeate-Lung02 phase 3 trial (TPS8126) evaluating ifinatamab deruxtecan (I-DXd) in patients with relapsed small cell lung cancer, the REJOICE-Ovarian01 phase 2/3 trial (TPS5625) evaluating raludotatug deruxtecan (R-DXd) in patients with platinum-resistant ovarian cancer, the HERTHENA-PanTumor01 phase 2 trial (TPS3164) evaluating patritumab deruxtecan (HER3-DXd) in patients with locally advanced or metastatic solid tumors, and the first-in-human phase 1/2 trial (TPS3165) of DS-3939 in patients with advanced solid tumors. Additional trials-in-progress featuring combinations of Daiichi Sankyo’s DXd ADCs and a novel medicine in development include a phase 1b trial (TPS4180) evaluating valemetostat, a dual inhibitor of EZH1 and EZH2, in combination with ENHERTU or datopotamab deruxtecan in patients with solid tumors and a phase 1b trial (TPS1120) evaluating valemetostat in combination with ENHERTU in HER2 low, ultralow and null metastatic breast cancers. Daiichi Sankyo will hold a virtual conference call for investors on Monday, June 3, 2024 from 6:00 to 7:00 pm CDT / Tuesday, June 4, 2024 from 8:00 to 9:00 am JST. Executives from Daiichi Sankyo will provide an overview of the ASCO research data and address questions. Highlights of data from Daiichi Sankyo’s oncology portfolio at ASCO 2024 include: Presentation Title Author Abstract Presentation (CDT) ENHERTU (trastuzumab deruxtecan; T-DXd) Breast Trastuzumab deruxtecan (T-DXd) vs physician’s choice of chemotherapy (TPC) in patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2 (HER2) low or HER2 ultralow metastatic breast cancer (mBC) with prior endocrine therapy (ET): primary results from DESTINY-Breast06 (DB-06) G. Curigliano LBA1000 Oral Presentation Sunday, June 2 7:30 – 8:00 am Trastuzumab deruxtecan (T-DXd) vs trastuzumab emtansine (T-DM1) in patients with HER2+ mBC: updated survival results of DESTINY-Breast03 E. Hamilton 1025 Poster Session Sunday, June 2 9:00 am – 12:00 pm DESTINY-Breast07: dose-expansion interim analysis of T-DXd monotherapy and T-DXd + pertuzumab in patients with previously untreated HER2+ mBC F. Andre 1009 Oral Presentation Saturday, June 1 3:00 – 6:00 pm Pooled analysis by best confirmed response to trastuzumab deruxtecan (T-DXd) in patients with HER2+ mBC from DESTINY-Breast-01, 02, and 03 C. Saura 1023 Poster Session Sunday, June 2 9:00 am – 12:00 pm Lung Trastuzumab deruxtecan in patients with HER2 mutant metastatic non-small cell lung cancer: final analysis results of DESTINY-Lung02 P. Janne 8543 Poster Session Monday, June 3 1:30 – 4:30 pm Tumor Agnostic Trastuzumab deruxtecan (T-DXd) in patients with HER2 expressing biliary tract cancer and pancreatic cancer: outcomes from DESTINY-PanTumor02 D. Oh 4090 Poster Session Saturday, June 1 1:30 – 4:30 pm Efficacy and safety of trastuzumab deruxtecan (T-DXd) in patients with HER2 expressing solid tumors: results from the bladder cohort of DESTINY-PanTumor02 study P. Wysocki 4565 Poster Session Sunday, June 2 9:00 am – 12:00 pm Trastuzumab deruxtecan (T-DXd) in patients with HER2 expressing head and neck tumors: outcomes from DESTINY-PanTumor02 F. Meric-Bernstam 6037 Poster Session Monday, June 3 9:00 am – 12:00 pm Datopotamab Deruxtecan (Dato-DXd) Breast Datopotamab deruxtecan versus chemotherapy in previously treated inoperable or metastatic hormone receptor positive, HER2 negative breast cancer: Patient-reported outcomes from the TROPION-Breast01 study S. Pernas 1006 Oral Presentation Saturday, June 1 3:00 – 6:00 pm Lung Datopotamab deruxtecan plus pembrolizumab with or without platinum chemotherapy as first-line therapy for advanced non-small cell lung cancer: subgroup analysis from TROPION-Lung02 B. Levy 8617 Poster Session Monday, June 3 1:30 – 4:30 pm Intracranial efficacy of datopotamab deruxtecan in patients with previously treated advanced/metastatic non-small cell lung cancer with actionable genomic alterations: results from TROPION-Lung05 A. Lisberg 8593 Poster Session Monday, June 3 1:30 – 4:30 pm Patritumab Deruxtecan (HER3-DXd) Pan-Tumor HERTHENA-PanTumor01: a global, multicohort phase 2 trial of HER3-DXd in relapsed/refractory metastatic solid tumors A. Bhatia TPS3164 Poster Session Saturday, June 1 9:00 am -12:00 pm Patritumab deruxtecan (HER3-DXd) in active brain metastases from metastatic breast and non–small cell lung cancers, and leptomeningeal disease from advanced solid tumors: the TUXEDO-3 phase II trial R. Bartsch TPS2091 Poster Session Saturday, June 1 9:00 am -12:00 pm Ifinatamab Deruxtecan (I-DXd) Lung IDeate-Lung02: a phase 3, randomized, open-label study of ifinatamab deruxtecan (I-DXd) vs treatment of physician’s choice in relapsed small cell lung cancer T. Owonikoko TPS8126 Poster Session Monday, June 3 1:30 – 4:30 pm Raludotatug Deruxtecan (R-DXd) Ovarian REJOICE-Ovarian01: a phase 2/3 study of raludotatug deruxtecan (R-DXd) in patients with platinum-resistant ovarian cancer I. Ray-Coquard TPS5625 Poster Session Monday, June 3 9:00 am –12:00 pm DS-3939 Pan-Tumor A phase 1/2, first-in-human study of DS-3939 in patients with advanced solid tumors: a new DXd ADC targeting TA-MUC1 N. Yamamoto TPS3165 Poster Session Saturday, June 1 9:00 am – 12:00 pm Valemetostat with DXd ADCs Breast Phase 1b study of EZH1/2 inhibitor valemetostat in combination with trastuzumab deruxtecan in patients with HER2 low/ultra low/null metastatic breast cancer T. Iwase TPS1120 Poster Session Sunday, June 2 9:00 am – 12:00 pm Pan-Tumor A phase 1b, multicenter, open-label study of valemetostat in combination with DXd antibody drug conjugates, trastuzumab deruxtecan (T-DXd) or datopotamab deruxtecan (Dato-DXd), in patients with solid tumors J. Sands TPS4180 Poster Session Saturday, June 1 1:30 – 4:30 pm About the DXd ADC Portfolio of Daiichi Sankyo The DXd ADC portfolio of Daiichi Sankyo currently consists of six ADCs in clinical development across multiple types of cancer. ENHERTU, a HER2 directed ADC, and datopotamab deruxtecan (Dato-DXd), a TROP2 directed ADC, are being jointly developed and commercialized globally with AstraZeneca. Patritumab deruxtecan (HER3-DXd), a HER3 directed ADC, ifinatamab deruxtecan (I-DXd), a B7-H3 directed ADC, and raludotatug deruxtecan (R-DXd), a CDH6 directed ADC, are being jointly developed and commercialized globally with Merck. DS-3939, a TA-MUC1 directed ADC, is being developed by Daiichi Sankyo. Designed using Daiichi Sankyo’s proprietary DXd ADC Technology to target and deliver a cytotoxic payload inside cancer cells that express a specific cell surface antigen, each ADC consists of a monoclonal antibody attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers. Datopotamab deruxtecan, ifinatamab deruxtecan, patritumab deruxtecan, raludotatug deruxtecan and DS-3939 are investigational medicines that have not been approved for any indication in any country. Safety and efficacy have not been established. About Daiichi Sankyo Daiichi Sankyo is an innovative global healthcare company contributing to the sustainable development of society that discovers, develops and delivers new standards of care to enrich the quality of life around the world. With more than 125 years of experience, Daiichi Sankyo leverages its world-class science and technology to create new modalities and innovative medicines for people with cancer, cardiovascular and other diseases with high unmet medical needs. For more information, please visit .

ASCOPhase 2Phase 1Phase 3Clinical Result

100 Deals associated with Valemetostat Tosilate

External Link

KEGG	Wiki	ATC	Drug Bank
D11551	-	-	-

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Adult T-Cell Leukemia-Lymphoma	JP	Daiichi Sankyo Co., Ltd.	26 Sep 2022
Peripheral T-Cell Lymphoma	JP	Daiichi Sankyo Co., Ltd.	26 Sep 2022

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Follicular Lymphoma	Phase 2	US	Daiichi Sankyo Co., Ltd.	19 May 2023
B-Cell Lymphoma	Phase 2	EU	Daiichi Sankyo Co., Ltd.	30 Jan 2022
B-cell lymphoma refractory	Phase 2	BE	Daiichi Sankyo Co., Ltd.	11 Jun 2021
B-cell lymphoma refractory	Phase 2	FR	Daiichi Sankyo Co., Ltd.	11 Jun 2021
Small cell lung cancer recurrent	Phase 2	US	Memorial Sloan Kettering Cancer Center	15 Mar 2019
Advanced Malignant Solid Neoplasm	Phase 1	US	Daiichi Sankyo Co., Ltd.	16 Feb 2024
Advanced Malignant Solid Neoplasm	Phase 1	JP	Daiichi Sankyo Co., Ltd.	16 Feb 2024
Castration-Resistant Prostatic Cancer	Phase 1	US	National Cancer Institute	20 Aug 2020
Metastatic Clear Cell Renal Cell Carcinoma	Phase 1	US	National Cancer Institute	20 Aug 2020
Metastatic Solid Tumor	Phase 1	US	National Cancer Institute	20 Aug 2020

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06244485 (ASCO2024)	Phase 1	Solid tumor SLFN11 \| HER2-positive	70	Valemetostat + T-DXd	fowonmdrvg(qrjsiutjoe) = wljxurmfci vekvwtglxf (bnkuxfrhre )	-	24 May 2024
NCT06244485 (ASCO2024)	Phase 1	Solid tumor SLFN11 \| HER2-positive	70	Valemetostat + Dato-DXd	fowonmdrvg(qrjsiutjoe) = lknwnmvngz vekvwtglxf (bnkuxfrhre )	-	24 May 2024
NCT02732275 (DS3201-A-J101, EHA2024) Manual	Phase 1	Non-Hodgkin Lymphoma EZH2 mutation	90	valemetostat (PTCL)	tlnhvshnrm(xpkdpftlnq) = yhowobikkx yvwtskcqiy (fwwjamorbv ) View more	Positive	14 May 2024
NCT02732275 (DS3201-A-J101, EHA2024) Manual	Phase 1	Non-Hodgkin Lymphoma EZH2 mutation	90	valemetostat (ATLL)	uiyimzkmsn(hqgmxfnnqt) = qqfjizvpdf uzwfodgnnf (ketddwvqqs, 1.4 - 38.7) View more	Positive	14 May 2024
NCT03110354 (CTgov)	Phase 1	Acute Myeloid Leukemia \| Acute Lymphoblastic Leukemia	28	DS-3201b (DS-3201b 150 mg)	anefhajsto(khlgpfydmw) = iimpaqythl klwicjllwm (mmoooafalv, gumpykxrdb - eytwrfixgf) View more	-	30 Jan 2024
NCT03110354 (CTgov)	Phase 1	Acute Myeloid Leukemia \| Acute Lymphoblastic Leukemia	28	DS-3201b (DS-3201b 250 mg)	anefhajsto(khlgpfydmw) = xccytiuhgu klwicjllwm (mmoooafalv, ovhgvnlrvr - osijcoctqr) View more	-	30 Jan 2024
ASH2023	Phase 1	Peripheral T-Cell Lymphoma	71	Valemetostat	wpyvjjrpny(hbbicfdnbu) = nhplmhyfqe sfrvhhdhut (sdxsdraxsd ) View more	-	09 Dec 2023
VALENTINE-PTCL01 (ASH2023)	Phase 2	Peripheral T-Cell Lymphoma	133	Valemetostat 200 mg/day	avzcqhiymw(fanqefdnum) = hlvowaqsiz trxwwavkfo (trbaezzpzo, 34.6 - 53.1) View more	-	09 Dec 2023
ASH2023	Phase 1	B-cell lymphoma refractory	19	Valemetostat	vmqbigybai(zfctpoubsc) = The most common TEAEs (any grade) were decreased platelet count (64%), dysgeusia (50%), anemia (43%), decreased neutrophil count (34%), and alopecia (33%) hcstyzyjos (xpgxevztjn ) View more	-	09 Dec 2023
NCT04102150 (VALENTINE-PTCL01, Pubmed) Manual	Phase 2	Adult T-Cell Leukemia-Lymphoma	25	Valemetostat Tosilate	frfwidhinu(aygnrwgnhd) = kmbkpaqnuk qcyqzuweme (cdfryvkrrx, 30.5 - 65.9) View more	Positive	23 Sep 2022
NCT04102150 (VALENTINE-PTCL01, ASH2021) Manual	Phase 2	Adult T-cell lymphoma/leukaemia refractory	25	Valemetostat Tosylate	ozpgsftzcx(zufkkcxlzm) = jdypvwdyhy yrupxbffow (cytygprsnz, 27.8 - 68.7) View more	Positive	05 Nov 2021
NCT02732275 (phase 1 trial, ICML2021)	Phase 1	Non-Hodgkin Lymphoma EZH2 \| EZH1	78	Valemetostat tosylate (DS-3201b)	fbrpvykmgl(syksjcvbdl) = jxwzjbchdl hulchakrlc (sxcufyblqp ) View more	Positive	17 Jun 2021

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Leverages most recent intelligence information, enabling fullest potential.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis