IP Library › Granted Patent US 12,364,761
Granted Patent B2
US 12,364,761 · App. 18/749,522 · Granted Jul 22, 2025

Dosages of immunoconjugates of antibodies and SN-38 for improved efficacy and decreased toxicity

Inventors: Serengulam V. Govindan (Springfield, NJ); David M. Goldenberg (Delray Beach, FL)
Assignee: IMMUNOMEDICS, INC.
A61K45/06A61K31/337A61K31/4184A61K31/4375A61K31/454A61K31/4745A61K31/513A61K31/675A61K31/7088A61K31/713A61K33/243A61K47/6803A61K47/6849A61K47/6851A61K47/6853C07K16/2803C07K16/2833C07K16/2887C07K16/30C07K16/3007C07K16/3046C07K2317/24C07K2317/565C07K2317/732C07K2317/92C07K2317/94
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Quick Facts
Patent No.
US 12,364,761
App. No.
18/749,522
Granted
Jul 22, 2025
Kind
B2
Abstract

The present invention relates to therapeutic immunoconjugates comprising SN-38 attached to an anti-Trop-2 antibody or antigen-binding antibody fragment. In preferred embodiments, the antibody may be an hRS7 antibody. The methods and compostions are of use to treat Trop-2 expressing cancers in human patients, preferably in patients who are resistant to or relapsed from at least one prior anti-cancer therapy, more preferably in patients who are resistant to or relapsed from treatment with irinotecan. The immunoconjugate may be administered at a dosage of 3 mg/kg to 18 mg/kg, preferably 8 to 12 mg/kg, more preferably 8 to 10 mg/kg. When administered at specified dosages and schedules, the immunoconjugate can reduce solid tumors in size and reduce or eliminate metastases. Preferred tumors to treat with the subject immunoconjugates include triple-negative breast cancer, HER+, ER+, progesterone+ breast cancer, metastatic non-small-cell lung cancer, a metastatic small-cell lung cancer and metastatic pancreatic cancer.

Claims (16)

1. A method of treating refractory breast cancer comprising administering to a human patient with refractory breast cancer an immunoconjugate sacituzumab govitecan (IMMU-132), wherein the immunoconjugate is administered to the human patient on Day 1 and Day 8 of a 21-day cycle; wherein the immunoconjugate is administered at a dosage between 8 and 10 mg/kg; and wherein the patient has received at least one prior therapy.

2. The method of claim 1 , wherein the refractory breast cancer is metastatic.

3. The method of claim 1 , wherein the immunoconjugate is administered at a dosage of 8 mg/kg, 9 mg/kg, or 10 mg/kg.

4. The method of claim 3 , wherein the immunoconjugate is administered at a dosage of 10 mg/kg.

5. The method of claim 1 , wherein the patient has received at least two prior therapies.

6. The method of claim 5 , wherein the patient has received three or more prior therapies.

7. The method of claim 6 , wherein at least two of the prior therapies are systemic therapies in a metastatic setting.

8. The method of claim 7 , wherein the prior systemic therapy is selected from the group consisting of cyclophosphamide, doxorubicin, carboplatin, gemcitabine, capecitabine, eribulin, cisplatinum, anastrozole, vinorelbine, bevacizumab, tamoxifen and taxane.

9. The method of claim 1 , wherein the cycle is repeated 4, 6, 8, 10, 12, 16 or 20 times.

10. The method of claim 1 , wherein the cycle is repeated until dose-limiting toxicity or progression.

11. A method of treating refractory breast cancer comprising administering to a human patient with metastatic breast cancer an immunoconjugate sacituzumab govitecan (IMMU-132), wherein the immunoconjugate is administered at a dosage between 8 and 10 mg/kg, wherein the patient has received three or more prior therapies, at least two of the prior therapies are systemic therapies for in the metastatic setting, and wherein the immunoconjugate dosage is administered to the human patient at Day 1 and Day 8 of a 21-day cycle.

12. The method of claim 11 , wherein the immunoconjugate is administered at a dosage of 8 mg/kg, 9 mg/kg, or 10 mg/kg.

13. The method of claim 12 , wherein the immunoconjugate is administered at a dosage of 10 mg/kg.

14. The method of claim 13 , wherein the prior systemic therapy is selected from the group consisting of cyclophosphamide, doxorubicin, carboplatin, gemcitabine, capecitabine, eribulin, cisplatinum, anastrozole, vinorelbine, bevacizumab, tamoxifen and taxane.

15. The method of claim 11 , wherein the cycle is repeated 4, 6, 8, 10, 12, 16 or 20 times.

16. The method of claim 11 , wherein the cycle is repeated until dose-limiting toxicity or progression.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 24, 2024
From: GOVINDAN, SERENGULAM V.; GOLDENBERG, DAVID M.
To: IMMUNOMEDICS, INC.
Reel/Frame 069009/0590 →
Continuity (15)
Continuation 18473133 · Sep 22, 2023
Continuation 18313830 · May 8, 2023
Continuation 17077229 · Oct 22, 2020
Division 16155423 · Oct 9, 2018
Division 15069208 · Mar 14, 2016
Continuation In Part 14667982 · Mar 25, 2015
Division 13948732 · Jul 23, 2013
Provisional Application 62241881 · Oct 15, 2015
Provisional Application 62156608 · May 4, 2015
Provisional Application 62133654 · Mar 16, 2015
Provisional Application 62133729 · Mar 16, 2015
Provisional Application 61749548 · Jan 7, 2013
Provisional Application 61736684 · Dec 13, 2012
Provisional Application 62138092 · Mar 25, 2015
Related Publication 20240398955A1 · Dec 5, 2024
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