Tinostamustine Scientific Publications

The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101

Anti-Cancer Agents in Medicinal Chemistry. 2016;16(1):20-28

Mehrling T, Chen Y

Fusion Therapy. A New Approach to Combining Treatments. Drug Discovery World.

Drug Discovery World. 2016; Fall.

Mehrling T.

Chemotherapy is Getting 'Smarter.'

Future Oncology. 2015;11(4):549-552.

Mehrling T.

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.

Qiu Y, Li Z, Copland JA, Mehrling T, Tun HW.

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.

Festuccia C, Mancini A, Colapietro A, et al.

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).

Festuccia C, Mancini A, Colapietro A, et al.

Is There Hope to Treat Glioblastoma Effectively?

CNS Oncol. 2015;4(6):377-379.

Mehrling T.

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.

Roth P, Moreno Candilejo I, Vaz Salgado MA, et al.

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.

Mehrling T, Ricevuto E, Gravina GL, Mancini A, Festuccia C.

Safety and Efficacy of Tinostamustine in a Subpopulation of Patients with Relapsed Refractory Hodgkins Lymphoma Phase 1 Study.

Hematological Oncology. 2025;43:e70000.

Sureda A, Pinto A, Ghesquieres H, et al.

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.

M’kacher R, Frenzel M, Jawhar MA, et al.

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.

Zinzani PL, Morschhauser F, Janik T, Manamley N, Hilgier K, Balari AMS.

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.

Sureda AM, Ghesquieres H, Morschhauser F, et al.

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.

Sureda A, Pinto A, Ghesquieres H, et al.

Safety and Efficacy of Tinostamustine in Heavily Pre-Treated Patients with Relapsed/Refractory (R/R) Hodgkin Lymphoma (HL).Safety and Efficacy of Tinostamustine in Heavily Pre-Treated Patients with Relapsed/Refractory (R/R) Hodgkin Lymphoma (HL).

Blood. 2021;138(S1):2472.

Ghesquieres H, Pinto A, Sureda A, et al.

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.

Lopez-Iglesias A, San-Segundo L, Gonzalez-Mendez L, et al.

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.

Kraus M, Bader J, Mehrling T, Driessen C.

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.

Díaz-Tejedor A, Rodríguez-Ubreva J, Ciudad L, et al.

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.

Besse L, Kraus M, Besse A, Bader J, Mehrling T, Driessen C.

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.

Lu Y, Jiang X, Li Y, et al.

Novel SAHA bendamustine Hybrid NL-101 in Combination with Daunorubicin Synergistically Suppresses Acute Myeloid Leukemia.

Oncology Reports. 2020;44:273-282.

Jin J, Li X, Guo W, et al.

Reinstated p53 Response and High Anti-T-Cell Leukemia Activity by the Novel Alkylating Deacetylase Inhibitor Tinostamustine.

Leukemia. 2020;34:2513–2518.

Pützer S, Varghese L, Von Jan J, et al.

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.

Jin J, Mao S, Li F, et al.

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.

Li X, Li C, Jin J, et al.

A Novel SAHA-Bendamustine Hybrid Induces Apoptosis of Leukemia Cells.

Oncotarget. 2015;6(24): 20121-20131.

Yu J, Qiu S, Ge Q, et al.

Effect and Mechanism of NL-101 Combined with Bcl-2 Inhibitor Venetoclax in Acute Myeloid Leukemia.

Blood. 2023;142(S1):2920–2922.

Jiang X, Zhuang H, Li F, Jiang L, Jin J, Lu Y.

A Phase I Study of Tinostamustine in Patients (pts) with Advanced Solid Tumours. Annals of Oncology.

Ann Oncol. 2019;30 (S5):470p.

Mita A, Loeffler M, Bui N, et al.

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.

Tinker AV, Chugh R, Curigliano G, et al.

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.

Chugh R, Kummar S, Schneider RE, et al.

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.

Yan S, Xu K, Lin J, et al.

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.

Joerger M, Diem S, Wyss N, et al.

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.

Joerger M, Diem S, Wyss n, et al.

Alkylating Histone Deacetylase Inhibitors May Have Therapeutic Value in Experimental Myeloperoxidase-ANCA Vasculitis.

Kidney Int. 2018;94(5):926-936.

Dooley D, Van Timmeren MM, O’Reilly VP, et al.

Combination Therapy with Checkpoint Inhibitors and Histone Deacetylase Inhibitors or Alkylating Agents.

Cancer Manag Res. 2024;16:855-869.

Joerger M, Koster KL, Janik T, de Jong FA.