Conjugates for treating diseases caused by PSMA expressing cells

• US 9,782,493 B2
• Filed: 08/24/2016
• Issued: 10/10/2017
• Est. Priority Date: 11/15/2012
• Status: Active Grant

• Current Assignee: Endocyte, Inc. (Novartis Ag)
• Original Assignee: Endocyte, Inc. (Novartis Ag)
• Inventors: Vlahov, Iontcho Radoslavov, Reddy, Joseph Anand, Bloomfield, Alicia, Dorton, Ryan, Nelson, Melissa, Vetzel, Marilynn, Leamon, Christopher Paul
• Primary Examiner(s): Ha, Julie
• Assistant Examiner(s): KOMATSU, LI N
• Application Number:
  US15/245,505
• Publication Number:
  US 20160361376A1
• Time in Patent Office: 412 Days
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61K 38/05 Dipeptides
• CPC Class Codes: A61K 38/06 Tripeptides
• CPC Class Codes: A61K 38/07 Tetrapeptides
• CPC Class Codes: A61K 38/08 Peptides having 5 to 11 amino acids A61K38/043 - A61K38/046 take precedence
• CPC Class Codes: A61K 47/542 Carboxylic acids, e.g. a fatty acid or an amino acid
• CPC Class Codes: A61K 47/547 Chelates, e.g. Gd-DOTA or Zinc-amino acid chelates; Chelate-forming compounds, e.g. DOTA or ethylenediamine being covalently linked or complexed to the pharmacologically- or therapeutically-active agent
• CPC Class Codes: A61K 47/64 Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent peptidic linkers A61K47/65
• CPC Class Codes: A61K 49/0002 General or multifunctional contrast agents, e.g. chelated agents
• CPC Class Codes: A61K 51/04 Organic compounds
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 13/10 of the bladder
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07K 5/021 containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
• CPC Class Codes: C07K 5/06113 Asp- or Asn-amino acid
• CPC Class Codes: C07K 5/10 Tetrapeptides
• CPC Class Codes: C07K 5/1019 with the first amino acid being basic

Abstract

The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

Claims

1. A method of treating prostate cancer in a patient, comprising administering a therapeutically effective amount of a conjugate having a formula

2. A method of treating prostate cancer in a patient, comprising administering a composition comprising a therapeutically effective amount of a conjugate having a formula

3. The method of claim 2, wherein the patient is a human.

4. The method of claim 2, wherein the composition is administered to the patient in an oral dosage form.

5. The method of claim 4, wherein the oral dosage form is selected from the group consisting of a tablet, a capsule, an elixir, and a syrup.

6. The method of claim 2, wherein the composition is administered to the patient in a parenteral dosage form.

7. The method of claim 6, wherein the parenteral dosage form is administered to the patient through a route selected from the group consisting of intravenous, intraarterial, intraperitoneal, epidurial, intraurethral, intrasternal, intramuscular, and subcutaneous.

8. The method of claim 2, wherein the therapeutically effective amount is from about 1 μ

g/kg to about 1 g/kg.

9. The method of claim 2, wherein the therapeutically effective amount is administered in a single dosage.

10. The method of claim 2, wherein the therapeutically effective amount is administered in a divided dosage.

11. The method of claim 2, wherein the therapeutically effective amount is administered once daily.

12. The method of claim 2, wherein the therapeutically effective amount is administered twice daily.

13. The method of claim 2, wherein the therapeutically effective amount is administered thrice daily.

14. The method of claim 2, wherein the therapeutically effective amount is administered once a week.

15. The method of claim 2, wherein the therapeutically effective amount is administered once a month.

16. The method of claim 2, wherein the therapeutically effective amount is administered once a quarter.

17. The method of claim 2, wherein the composition further comprises a pharmaceutically-acceptable carrier, a pharmaceutically-acceptable adjuvant, a pharmaceutically-acceptable vehicle, a pharmaceutically-acceptable excipient, or a combination thereof.

18. The method of claim 2, wherein the composition is in a form selected from the group consisting of a tablet, a pill, a powder, a lozenge, a sachet, a cachet, an elixir, a suspension, an emulsion, a solution, a syrup, a solid aerosol, an aerosol in a liquid medium, an ointment, a soft gelatin capsule, a hard gelatin capsule, and a suppository.

19. The method of claim 18, wherein the composition is in a form selected from the group consisting of a sterile injectable solution and a sterile packaged powder.