IP Library Granted Patent US 12,239,636
Granted Patent B2
US 12,239,636 · App. 17/274,725 · Granted Mar 4, 2025

Combined sirolimus and nintedanib therapy for vascular lesions and hereditary hemorrhagic telangiectasia

Inventor: Philippe Marambaud (Astoria, NY)
Assignee: THE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
A61K31/436A61K31/496A61P7/04A61P7/06
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Quick Facts
Patent No.
US 12,239,636
App. No.
17/274,725
Granted
Mar 4, 2025
Kind
B2
Abstract

Methods and pharmaceutical compositions comprising one or more mTOR inhibitors such as sirolimus and one or more receptor tyrosine kinase inhibitors such as nintedanib are disclosed for treating vascular lesions and hereditary hemorrhagic telangiectasia.

Claims (24)

1. A method of treating one or more of an arteriovenous malformation, a vascular lesion and bleeding in a subject who has hereditary hemorrhagic telangiectasia (HHT) comprising administering to the subject sirolimus and nintedanib in therapeutically effective amounts to treat an arteriovenous malformation, a vascular lesion and/or bleeding in the subject, wherein sirolimus and nintedanib are the only therapeutic agents administered to the subject.

2. A method of treating hereditary hemorrhagic telangiectasia (HHT) in a subject in need thereof comprising administering to the HHT subject sirolimus and nintedanib in therapeutically effective amounts to treat abnormal blood vessel formation in the subject, wherein sirolimus and nintedanib are the only therapeutic agents administered to the subject.

3. The method of claim 1 , wherein sirolimus and nintedanib are co-administered to the subject.

4. The method of claim 3 , wherein sirolimus and nintedanib are co-administered in the same formulation.

5. The method of claim 1 , wherein sirolimus and nintedanib are administered sequentially.

6. The method of claim 5 , wherein sirolimus and nintedanib are administered within 24 hours of each other.

7. The method of claim 1 , wherein tacrolimus is administered to the subject in a therapeutically effective amount prior to administration of sirolimus and nintedanib.

8. The method of claim 1 , wherein administration is by oral administration, by nasal administration, by rectal administration or transdermally.

9. The method of claim 1 , wherein the subject is a human.

10. The method of claim 1 , wherein sirolimus is administered in a dose of 0.03-1 mg/kg body weight/day.

11. The method of claim 10 , wherein sirolimus is administered in a dose of 0.04 mg/kg body weight/day.

12. The method of claim 1 , wherein nintedanib is administered in a dose of 0.02-5 mg/kg body weight/day.

13. The method of claim 12 , wherein nintedanib is administered in a dose of 0.5 mg/kg body weight/day.

14. The method of claim 7 , wherein tacrolimus is administered in a dose of 0.03-1 mg/kg body weight/day.

15. The method of claim 1 , wherein bleeding occurs in the nose, oral mucosa, lung, liver, gastrointestinal tract, brain and/or retina.

16. The method of claim 2 , wherein sirolimus and nintedanib are co-administered to the subject.

17. The method of claim 16 , wherein sirolimus and nintedanib are co-administered in the same formulation.

18. The method of claim 2 , wherein sirolimus and nintedanib are administered sequentially.

19. The method of claim 18 , wherein sirolimus and nintedanib are administered within 24 hours of each other.

20. The method of claim 2 , wherein tacrolimus is administered to the subject in a therapeutically effective amount prior to administration of sirolimus and nintedanib.

21. The method of claim 2 , wherein the subject is a human.

22. The method of claim 2 , wherein sirolimus is administered in a dose of 0.03-1 mg/kg body weight/day.

23. The method of claim 2 , wherein nintedanib is administered in a dose of 0.02-5 mg/kg body weight/day.

24. The method of claim 20 , wherein tacrolimus is administered in a dose of 0.03-1 mg/kg body weight/day.

Assignments (1)
CONFIRMATORY LICENSE Recorded Nov 22, 2023
From: FEINSTEIN INSTITUTE FOR MEDICAL RESEARCH
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 065648/0444 →
Continuity (2)
Provisional Application 62736564 · Sep 26, 2018
Related Publication 20210346355A1 · Nov 11, 2021
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