IP Library Granted Patent US 12,527,811
Granted Patent B2
US 12,527,811 · App. 18/080,954 · Granted Jan 20, 2026

Defibrotide for the prevention and treatment of cytokine release syndrome and neurotoxicity associated with immunodepletion

Inventors: Sarah McMahon (Palo Alto, CA); Yasuhiro Oki (Palo Alto, CA)
Assignee: Paul G. Richardson
A61K31/711A61K39/0011A61P25/00G01N33/6896A61K2039/5156A61K2039/5158G01N2800/52
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Quick Facts
Patent No.
US 12,527,811
App. No.
18/080,954
Granted
Jan 20, 2026
Kind
B2
Abstract

The present disclosure provides method of preventing, lessening the effects, or treating cytokine release syndrome (CRS) or related disorders, and/or neurotoxicity associated with immunotherapy comprising administering defibrotide. The defibrotide can be administered after the immunotherapy begins or be administered prophylactically before immunotherapy begins or before the patient develops CRS and/or neurotoxicity.

Claims (37)

1 . A method of preventing and/or treating Cytokine Release Syndrome (CRS) in a patient in need thereof comprising administering a therapeutically effective amount of defibrotide.

2 . The method of claim 1 , wherein administration of defibrotide decreases serum biomarker levels associated with the development of CRS in the patient.

3 . The method of claim 1 further comprising determining whether to administer defibrotide to a patient comprising:

determining the expression of a biomarker associated with CRS.

4 . The method of claim 3 , wherein defibrotide is administered to the patient until

a) the serum biomarker levels decrease to levels observed in patients who do not develop CRS; or

b) the serum biomarker levels decrease to levels observed in the same patient before immunotherapy treatment.

5 . The method of claim 1 , wherein the patient is receiving or about to receive an immunotherapy, wherein the immunotherapy is selected from the group consisting of:

a) lymphodepletion chemotherapy;

b) a CAR-T therapy;

c) a monoclonal antibody; and

d) a bispecific antibody.

6 . The method of claim 5 , wherein defibrotide is administered

a) before the administration of the immunotherapy;

b) at the same time as the administration of the immunotherapy; or

c) after the administration of the immunotherapy.

7 . The method of claim 1 , wherein defibrotide is administered

a) before the development of CRS or symptoms thereof,

b) after the development of CRS or symptoms thereof; or

c) after the development of CRS or symptoms thereof and administration continues until symptoms improve.

8 . The method of claim 6 , wherein defibrotide is administered between one and three days before administration of the immunotherapy begins.

9 . The method of claim 8 , wherein administration of defibrotide continues up to 30 days.

10 . The method of claim 1 , wherein defibrotide is administered

a) at a dose between 1 mg/kg and 10 mg/kg; or

b) at a dose of 6.25 mg/kg.

11 . The method of claim 1 , wherein defibrotide is administered

a) once a day;

b) multiple doses per day;

c) in two to ten doses per day;

d) four times a day; or

e) every six hours.

12 . The method of claim 11 , wherein defibrotide is administered intravenously, every six hours at a dose of 6.25 mg/kg.

13 . The method of claim 2 , wherein the biomarker is selected from the group consisting of ILI-Ra, IL-6, IL-6R, soluble IL-6R, soluble gpl30, IFNa, IFNy, IL-15, IL-8, IL-2, SIL2Ra, IL8, IP10, MCP1, MIG, GM-CSF, TNFa, MIP-1a, MIPI and IL-10, anti-neuron autoantibodies, stress proteins, MAO and ChE enzyme activity, D2 receptor, mACh receptor, Hsp70, autoantibodies, c-fos expression, ornithine decarboxylase gene expression, cerebrospinal fluid markers, plasma components, IFNg, TNFRp55, Endothelin-1, soluble Vascular Cell Adhesion Molecule (VCAM), Intra-Cellular Adhesion Molecule (ICAM), E-selectin, soluble Thrombomodulin, Von Willebrand factor (vWF), DAMP (damage-associated molecular patterns), PAMP (pathogen-associated molecular patterns), and a combination thereof.

14 . The method of claim 13 , wherein the stress proteins are heat shock proteins.

15 . The method of claim 13 , wherein the plasma components are myelin basic protein, anti-NF, anti-myelin antibody, anti-GFAP antibody, or anti-nerve growth factor antibody.

16 . The method of claim 1 , wherein defibrotide is a high concentration defibrotide formulation.

17 . The method of claim 16 , wherein the high concentration defibrotide formulation comprises about 80 mg/mL to about 100 mg/mL of defibrotide and 10 mM to about 34 mM sodium citrate, and is formulated for subcutaneous delivery to the patient.

Assignments (4)
SECURITY AGREEMENT Recorded Jul 26, 2024
From: CAVION, INC.; CELATOR PHARMACEUTICALS, INC.; GW PHARMA LIMITED; JAZZ PHARMACEUTICALS, INC.; JAZZ PHARMACEUTICALS IRELAND LIMITED; JAZZ PHARMACEUTICALS RESEARCH UK LIMITED (F/K/A GW RESEARCH LIMITED)
To: U.S. BANK TRUST COMPANY, NATIONAL ASSOCIATION, AS COLLATERAL TRUSTEE
Reel/Frame 068173/0155 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 17, 2024
From: JAZZ PHARMACEUTICALS IRELAND LIMITED
To: RICHARDSON, PAUL G.
Reel/Frame 068005/0895 →
CORRECTIVE ASSIGNMENT TO CORRECT THE THE APPLICATION NUMBER PREVIOUSLY RECORDED AT REEL: 062735 FRAME: 0674. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Mar 31, 2023
From: MCMAHON, SARAH; OKI, YASUHIRO
To: JAZZ PHARMACEUTICALS, INC.
Reel/Frame 063361/0309 →
CORRECTIVE ASSIGNMENT TO CORRECT THE THE APPLICATION NUMBER PREVIOUSLY RECORDED AT REEL: 062735 FRAME: 0583. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Mar 31, 2023
From: JAZZ PHARMACEUTICALS, INC.
To: JAZZ PHARMACEUTICALS IRELAND LIMITED
Reel/Frame 063361/0328 →
Continuity (5)
Continuation 17046906
Provisional Application 62753711 · Oct 31, 2018
Provisional Application 62657161 · Apr 13, 2018
Provisional Application 62656486 · Apr 12, 2018
Related Publication 20230190784A1 · Jun 22, 2023
References Cited (36)
US 11571440B2 · McMahon · 2023 [cited by examiner]
US 20210187004A1 · McMahon et al. · 2021 [cited by applicant]
Defibrotide: (LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; Defibrotide. [Updated Dec. 27, 2017]). [cited by examiner]
Corbacioglu et al. (Biol Blood Marrow Transplant 22 (2016) 1874-1882). [cited by examiner]
Bagal et al. (Hematology/Oncology and Stem Cell Therapy 11(1):p. 47-51, Jan.-Mar. 2018). [cited by examiner]
Jacobson et al. (Blood Adv. Jul. 5, 2023;7(21):6790-6799). [cited by examiner]
Beşişik et al., “Complete resolution of transplantation-associated thrombotic microangiopathy and hepatic veno-occlusive disease by defibrotide and plasma exchange,” Turk J Gastroenterol 2005, 16(1): 34-37. [cited by applicant]
Benimetskaya et al., “Angiogenesis alteration by defibrotide: implications for its mechanism of action in severe hepatic veno-occlusive disease,” Blood, vol. 112, No. 10, Nov. 15, 2008, pp. 4343-4352. [cited by applicant]
Bonomini, V., et al., “Effect of a New Antithrombotic Agent (Defibrotide) in Acute Renal Failure Due to Thrombotic Microangiopathy,” Nephron, 1985, vol. 40(2), pp. 195-200. [cited by applicant]
ClinicalTrials.gov Identifier: NCT03954106, A Safety and Efficacy Study of Defibrotide in the Prevention of Chimeric Antigen Receptor-T-cell-associated Neurotoxicity, First Posted—May 17, 2019, Last Update Posted—Dec. 9… [cited by applicant]
ClinicalTrials.gov Identifier: NCT04348383, Defibrotide as Prevention and Treatment of Respiratory Distress and Cytokine Release Syndrome of Covid 19. (DEFACOVID), First Posted—Apr. 16, 2020, Last Update Posted—Dec. 9, … [cited by applicant]
Corbacioglu et al., “Defibrotide for the Treatment of Hepatic Veno-Occlusive Disease: Final Results From the International Compassionate-Use Program,” Biol Blood Marrow Transplant (2016) 22: 1874-1882. [cited by applicant]
Gentium S.r.l., Summary of Product Characteristics for Defitelio, Oct. 18, 2013, 25 pages. [cited by applicant]
International Search Report and Written Opinion of the International Searching Authority for International Application No. PCT/US2019/027210 dated Jul. 4, 2019,12 pages. [cited by applicant]
Jazz Pharmaceuticals: “Jazz Pharmaceuticals Announces First Patient Enrolled in EMERGE-201 Phase 2 Basket Trial Evaluating Zepzelca (Iurbinectedin) Monotherapy in Patients With Select Advanced or Metastatic Solid Tumors… [cited by applicant]
Johnson, G.L., et al., “Acute Renal Failure and Neurotoxicity Following Oral Acyclovir,” The Annals of Pharmacotherapy, Apr. 1994, vol. 28, pp. 460-463. [cited by applicant]
Mitsiades et al., “Defibrotide (OF), an Orally Bioavailable Modulator of Myeloma Tumor-Microenvironment Interactions: Molecular Sequelae and Clinical Implications,” Blood, 2006, 108: 3523, 6 pages. [cited by applicant]
Sala et al., “Polydeoxyribonucleotide (defibrotide) protects against post-ischemic behavioral, electroencephalographic and neuronal damage in the gerbil,” European Journal of Pharmacology (1997) 328: 143-152. [cited by applicant]
Vangelista et al., “Effects of Defibrotide in Acute Renal Failure due to Thrombotic Microangiopathy,” Haemostasis (1986) 16: Suppl. 1, pp. 51-54. [cited by applicant]
Frame, D. et al., “Defibrotide Therapy for SARS-CoV-2 Ards” Chest. (Aug. 2022) pp. 346-355, vol. 162, No. 2. [cited by applicant]
Richardson, E. et al., “Defibrotide: potential for treating endothelial dysfunction related to viral and post-infectious syndromes” Expert Opin Ther Targets. (Jun. 2021) pp. 423-433, vol. 25, No. 6. [cited by applicant]
Ruggeri, A. et al., “Use of defibrotide in COVID-19 pneumonia: comparison of a phase II study and a matched real-world cohort control” Haematologica (Oct. 2024) pp. 3261-3268, vol. 109. [cited by applicant]
Mo, C. et al., “Endothelial injury and dysfunction with emerging immunotherapies in multiple myeloma, the impact of COVID-19, and endothelial protection with a focus on the evolving role of defibrotide” Blood Reviews (J… [cited by applicant]
Richardson, P. et al., “Safety and efficacy of defibrotide for the treatment of severe hepatic veno-occlusive disease” Ther Adv Hematol. (Aug. 2012) pp. 253-265, vol. 3, No. 4. [cited by applicant]
Richardson, P. et al., “Defibrotide sodium for the treatment of hepatic veno-occlusive disease/sinusoidal obstruction syndrome” Expert Rev Clin Pharmacol. (Feb. 2018) pp. 113-124, vol. 11, No. 2. [cited by applicant]
Martin, P. et al., “Pooled Dose Response Analysis of Defibrotide in >1600 Patients for the Treatment of Hepatic Veno-Occlusive Disease/Sinusoidal Obstruction Syndrome” Proceedings of the 2016 BMT Tandem Meetings (Feb. 2… [cited by applicant]
Arai, S. et al., “Efficacy and Safety of Defibrotide in a Subset Analysis of Late-Onset Hepatic Veno-Occlusive Disease/ Sinusoidal Obstruction Syndrome (VOD/SOS) Patients from an Ongoing, Expanded-Access Program” Procee… [cited by applicant]
Richardson, P. et al., “Adults Receiving Defibrotide for the Treatment of Hepatic Veno-Occlusive Disease/Sinusoidal Obstruction Syndrome (VOD/SOS) after Hematopoietic Stem Cell Transplantation (HSCT): Final Results from… [cited by applicant]
Richardson, P. et al., “Treatment of Severe Veno-Occlusive Disease With Defibrotide: Compassionate Use Results in Response Without Significant Toxicity in a High-Risk Population” Blood (Aug. 1998) pp. 737-744, vol. 92, … [cited by applicant]
Corbacioglu, S. et al., “Defibrotide for the treatment of hepatic veno-occlusive disease in children after hematopoietic stem cell transplantation” Expert Rev Hematol. (Jun. 2012) pp. 291-302, vol. 5, No. 3. [cited by applicant]
Richardson, P. et al., “Defibrotide for the treatment of hepatic veno-occlusive disease/sinusoidal obstruction syndrome with multiorgan failure” Int J Hematol Oncol. (Nov. 2017) pp. 75-93, vol. 6, No. 3. [cited by applicant]
Richardson, P. et al., “The use of defibrotide in blood and marrow transplantation” Blood Adv. (Jun. 2018) pp. 1495-1509, vol. 2, No. 12. [cited by applicant]
Richardson, P. et al., “Multi-institutional use of defibrotide in 88 patients after stem cell transplantation with severe veno-occlusive disease and multisystem organ failure: response without significant toxicity in a … [cited by applicant]
Richardson, P. et al., “Defibrotide for the treatment of severe hepatic veno-occlusive disease and multi-organ failure post stem cell transplantation: a multi-center, randomized, dose-finding trial” Biol Blood and Marro… [cited by applicant]
Richardson, P. et al., “Phase 3 trial of defibrotide for the treatment of severe veno-occlusive disease and multi-organ failure” Blood. (Mar. 2016) pp. 1656-1665, vol. 127, No. 13. [cited by applicant]
Kocoglu, M.H. et al., “Defibrotide improves COVID-19-related acute respiratory distress syndrome in myeloma patients after chimeric antigen receptor T-cell treatment without compromising virus-specific and anti-myeloma … [cited by applicant]