The below scientific publications discuss investigational uses of agents in development and are for informational and educational purposes only. They are not intended to convey conclusions about efficacy or safety. There is no guarantee that sunobinop or tinostamustine will successfully complete development or gain FDA approval.
Tinostamustine Scientific Publications
Introduction/Discovery
Manuscripts
| Date | Citation | Link |
|---|---|---|
| January 2016 | The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101. Anticancer Agents Med Chem. 2016;16(1):20-28. | Access Publication |
| October 2016 | Fusion Therapy. A New Approach to Combining Treatments. Drug Discovery World. Drug Discovery World. 2016; Fall. | Access Publication |
| February 2015 | Chemotherapy is Getting ‘Smarter’. Future Oncology. 2015;11(4):549-552. | Access Publication |
Glioblastoma
Manuscripts
| Date | Citation | Link |
|---|---|---|
| June 2018 | Combined Alkylation and Histone Deacetylase Inhibition with EDO-S101 Has Significant Therapeutic Activity Against Brain Tumors in Preclinical Models. Oncotarget. 2018;9(46):28155-28164. | Access Publication |
| March 2018 | Correction to: The First-In-Class Alkylating Deacetylase Inhibitor Molecule Tinostamustine Shows Antitumor Effects and is Synergistic with Radiotherapy in Preclinical Models of Glioblastoma. J Hematol Oncol. 2018;11(1):38. | Access Publication |
| February 2018 | The First-In-Class Alkylating Deacetylase Inhibitor Molecule Tinostamustine Shows Antitumor Effects and is Synergistic with Radiotherapy in Preclinical Models of Glioblastoma. J Hematol Oncol. 2018;v11(32). | Access Publication |
| October 2015 | Is There Hope to Treat Glioblastoma Effectively? CNS Oncol. 2015;4(6):377-379. | Access Publication |
Abstracts
| Date | Citation | Link |
|---|---|---|
| October 2025 | A Phase 1 Study of Tinostamustine, a Novel Alkylating Deacetylase Inhibitor, as an Adjunct Treatment in Newly Diagnosed MGMT Promoter-Unmethylated Glioblastoma. Neuro-Oncology. 2025; 27 (S3): iii116. | Access Publication |
| May 2015 | Activity of the Alkylating Histone-Deacetylase Inhibition Fusion Molecule EDO-S-101 in Preclinical Models of Human Glioblastoma Independent from MGMT Expression. Journal of Clinical Oncology. 2015;33:15_suppl:e13031-e13031. | Access Publication |
Hodgkin’s and non-Hodgkin’s Lymphomas
Manuscripts
| Date | Citation | Link |
|---|---|---|
| January 2025 | Safety and Efficacy of Tinostamustine in a Subpopulation of Patients with Relapsed Refractory Hodgkins Lymphoma Phase 1 Study. Hematological Oncology. 2025;43:e70000. | Access Publication |
| October 2018 | Establishment and Characterization of a Reliable Xenograft Model of Hodgkin Lymphoma Suitable for the Study of Tumor Origin and the Design of New Therapies. Cancers. 2018;10(414):2-28. | Access Publication |
Abstracts
| Date | Citation | Link |
|---|---|---|
| November 2023 | Results from the Cohort Expansion Stage of a Phase I Trial of Tinostamustine Monotherapy in Advanced Haematological Malignancies (NCT02576496): Findings from a Subset of Patients with Cutaneous T-cell Lymphoma (CTCL). Blood. 2023;142(S1):4432. | Access Publication |
| November 2023 | Results From the Cohort-Expansion Stage of a Phase I Trial of Tinostamustine Monotherapy in Advanced Hodgkin Lymphoma (HL), Non-Hodgkin Lymphoma (NHL) and Multiple Myeloma (MM) (NCT02576496). Blood. 2023;142(S1):4432. | Access Publication |
| November 2022 | Safety and Efficacy of Tinostamustine in Pre-Treated Patients with Relapsed/Refractory (R/R) Hodgkin Lymphoma (HL): Early Results from an Additional Expansion Cohort of a Phase I Study. Blood. 2022;140(S1):3696. | Access Publication |
| November 2021 | Safety and Efficacy of Tinostamustine in Heavily Pre-Treated Patients with Relapsed/Refractory (R/R) Hodgkin Lymphoma (HL). Blood. 2021;138(S1):2472. | Access Publication |
| December 2014 | The Alkylating Histone Deacetylase Inhibitor Fusion Molecule EDO-S1010 Displays Full Bi Functional Properties in Preclinical Models of Hematologic Malignancies. Blood. 2014;124(21):2100-2100. | Access Publication |
| December 2014 | EDO-S101, A New Alkylating Histone-Deacetylase Inhibitor (HDACI) Fusion Molecule, has Superior Activity Against Multiple Myeloma and B Cell Lymphoma and Strong Synergy with Proteasome Inhibitors In Vitro. Blood. 2014;124(21):2248. | Access Publication |
Myeloma
Manuscripts
| Date | Citation | Link |
|---|---|---|
| April 2024 | Tinostamustine (EDO-S101), an Alkylator and Histone Deacetylase Inhibitor, Enhances the Efficacy of Daratumumab in Multiple Myeloma by Upregulation of CD38 and NKG2D Ligands. Int J Molec Sci. 2024;25(9),4718. | Access Publication |
Abstracts
| Date | Citation | Link |
|---|---|---|
| December 2016 | The First in Class, Alkylator‑Histone‑Deacetylase‑Inhibitor Fusion Molecule EDO‑S101 in Combination with Proteasome Inhibitors Induces Highly Synergistic Pro‑Apoptotic Signaling Through UPS Activation and Suppression of c‑Myc and BCL2 in Multiple Myeloma. Blood. 2016;128(22):4466. | Access Publication |
| September 2015 | Preclinical Antimyeloma Activity of EDO-S101. Clinical Lymphoma, Myeloma and Leukemia. Clinical Lymphoma, Myeloma and Leukemia. 2015;15(A3):E218. | Access Publication |
| December 2014 | Identification of Novel Therapeutic Targets in the Clinically Predictive Vk*MYC Mouse Model of Multiple Myeloma. Blood. 2014;124(21):415. | Access Publication |
| December 2014 | The Alkylating Histone Deacetylase Inhibitor Fusion Molecule EDO-S101 Displays Full Bi-Functional Properties in Preclinical Models of Hematological Malignancies. Blood. 2014;124(21):2100. | Access Publication |
| December 2014 | EDO-S101, A New Alkylating Histone-Deacetylase Inhibitor (HDACI) Fusion Molecule, has Superior Activity Against Multiple Myeloma and B Cell Lymphoma and Strong Synergy with Proteasome Inhibitors In Vitro. Blood. 2014;124(21):2248. | Access Publication |
Leukemia
Manuscripts
| Date | Citation | Link |
|---|---|---|
| September 2024 | NL-101 Synergizes with the BCL‑2 Inhibitor Venetoclax Through PI3K‑Dependent Suppression of c‑Myc in Acute Myeloid Leukaemia. Journal of Translational Medicine. 2024;22:867. | Access Publication |
| April 2020 | Novel SAHA bendamustine Hybrid NL-101 in Combination with Daunorubicin Synergistically Suppresses Acute Myeloid Leukemia. Oncology Reports. 2020;44:273-282. | Access Publication |
| February 2020 | Reinstated p53 Response and High Anti-T-Cell Leukemia Activity by the Novel Alkylating Deacetylase Inhibitor Tinostamustine. Leukemia. 2020;34:2513–2518. | Access Publication |
| August 2019 | A Novel Alkylating Deacetylase Inhibitor Molecule EDO-S101 in Combination with Cytarabine Synergistically Enhances Apoptosis of Acute Myeloid Leukemia Cells. Med Oncol. 2019;36:77. | Access Publication |
| October 2018 | High PARP-1 Expression Predicts Poor Survival in Acute Myeloid Leukemia and PARP-1 Inhibitor and SAHA-Bendamustine Hybrid Inhibitor Combination Treatment Synergistically Enhances Anti-Tumor Effects. EBioMedicine. 2018;38:47-56. | Access Publication |
| October 2015 | A Novel SAHA-Bendamustine Hybrid Induces Apoptosis of Leukemia Cells. Oncotarget. 2015;6(24): 20121-20131. | Access Publication |
Abstracts
| Date | Citation | Link |
|---|---|---|
| November 2023 | Effect and Mechanism of NL-101 Combined with Bcl-2 Inhibitor Venetoclax in Acute Myeloid Leukemia. Blood. 2023;142(S1):2920–2922. | Access Publication |
Solid Tumors
Abstracts
| Date | Citation | Link |
|---|---|---|
| October 2019 | A Phase I Study of Tinostamustine in Patients (pts) with Advanced Solid Tumours. Annals of Oncology. Ann Oncol. 2019;30 (S5):470p. | Access Publication |
Ovarian Cancer
Abstracts
| Date | Citation | Link |
|---|---|---|
| 2023 | Results from a Phase I/II Trial of Tinostamustine Monotherapy in Advanced Solid Tumors (NCT03345485): Safety and Efficacy in a Subset of Patients with Advanced Ovarian Cancer (OVCA). Int J Gynecol Cancer 2023;33(Suppl 3):A163. | Access Publication |
Soft Tissue Sarcoma
Abstracts
| Date | Citation | Link |
|---|---|---|
| October 2023 | Results from a Phase I/II Trial of Tinostamustine Monotherapy in Advanced Solid Tumours (NCT03345485): Safety and Efficacy in a Subset of Patients (pts) with Soft Tissue Sarcoma (STS). Ann Oncol. 2023;34(S2):S1048. | Access Publication |
Small Cell Lung Cancer
Abstracts
| Date | Citation | Link |
|---|---|---|
| April 2012 | Synergistic Inhibition of Tumor growth and overcoming Chemo-Resistance Simultaneously Targeting Key Components of in DNA Damage Repair Epigenetic, Putative, Cancer Cell Signaling Pathways Using Novel Dual Functional DNA-Alkylating/HDAC Inhibitor and Tumor Suppressor Gene Nanoparticles in Lung Cancer. Cancer Research. 2012;72(8)(S1):2741. | Access Publication |
Advanced Melanoma
Manuscripts
| Date | Citation | Link |
|---|---|---|
| April 2025 | Open-Label Nonrandomized Phase IB Study to Characterize the Safety and Recommended Dose of Tinostamustine in Combination with Nivolumab in Patients with Advanced Melanoma (ENIgMA). Melanoma Research. 2025;35(4):252-258. | Access Publication |
Abstracts
| Date | Citation | Link |
|---|---|---|
| October 2023 | Open-Label Non-Randomized Phase IB Study to Characterize the Safety, Tolerability and Recommended Dose of Tinostamustine in Combination with Nivolumab in Patients with Advanced Melanoma (ENIGMA). Annals of Oncology. 2023; 34(S2): S662. | Access Publication |
ANCA Vasculitis
Manuscripts
| Date | Citation | Link |
|---|---|---|
| November 2018 | Alkylating Histone Deacetylase Inhibitors May Have Therapeutic Value in Experimental Myeloperoxidase-ANCA Vasculitis. Kidney Int. 2018;94(5):926-936. | Access Publication |
Combination with Checkpoint Inhibitors
Manuscripts (Review)
| Date | Citation | Link |
|---|---|---|
| July 2024 | Combination Therapy with Checkpoint Inhibitors and Histone Deacetylase Inhibitors or Alkylating Agents. Cancer Manag Res. 2024;16:855-869. | Access Publication |