Claims for Patent: 10,507,210

Summary for Patent: 10,507,210

Title:	Kinase inhibitor prodrug for the treatment of cancer
Abstract:	Compositions containing and methods of administering TH-4000 are useful in treatment of cancer alone or in combination with other anti-cancer agents.
Inventor(s):	Patterson; Adam Vorn (Auckland, NZ), Smaill; Jeffrey Bruce (Auckland, NZ), Silva; Shevan (Auckland, NZ), Guise; Christopher Paul (Auckland, NZ), Bull; Matthew Roy (Auckland, NZ), Jackson; Victoria (Auckland, NZ), Pearce; Tillman (South San Francisco, CA), Davar; Nipun (South San Francisco, CA)
Assignee:	Auckland UniServices Limited (Auckland, NZ)
Application Number:	15/531,677
Patent Claims:	1. A method of treating cancer in a subject in need thereof, said method comprising administering to the subject a therapeutically effective amount of a compound, [(E)-4-[[4-(3-bromo-4-chloroanilino)pyrido[3,4-d]pyrimidin-6-yl]amino]-4-- oxobut-2-enyl]-dimethyl-[(3-methyl-5-nitroimidazol-4-yl)methyl]azanium bromide, wherein said cancer is characterized by wild-type activity of the EGFR protein. 2. The method of claim 1, wherein the amount of the compound administered is in the range of about 20 mg/m.sup.2 to about 150 mg/m.sup.2. 3. The method of claim 1, wherein the compound is administered intravenously. 4. The method of claim 1, wherein the compound is administered at a frequency in the range of at least once per day to once per month. 5. The method of claim 1, wherein the compound is administered at a frequency of about once every three days. 6. The method of claim 1, wherein the compound is administered for a period of about 1 to about 60 weeks. 7. The method of claim 5, wherein the compound is administered about once every three days for about 24 days. 8. The method of claim 1, wherein the compound is administered over an infusion period of about 1 to about 6 hours. 9. The method of claim 1, wherein the cancer is relapsed or refractory or the patient is unsuitable for standard chemotherapy. 10. The method of claim 1, wherein the patient is also treated with erlotinib and/or cetuximab. 11. The method of claim 1, wherein the cancer treated is non-small cell lung cancer. 12. The method of claim 1, wherein the cancer treated is squamous cell cancer of the head and neck or skin. 13. The method of claim 1, wherein the compound is administered in a dosage unit comprising a pharmaceutically acceptable formulation of the compound. 14. The method of claim 13, wherein the pharmaceutically acceptable formulation comprises the compound or a pharmaceutically acceptable salt or solvate thereof and 2-hydroxylpropyl-3-cyclodextrin. 15. The method of claim 14, wherein the dosage unit comprises about 75 to about 150 mg of the compound. 16. The method of claim 1, wherein the compound is administered in a dose of about 150 mg/m.sup.2. 17. The method of claim 1, wherein the cancer is heterozygous for the EGFR protein. 18. The method of claim 17, wherein the cancer is characterized by a genotype comprising one mutant EGFR allele and one wild-type EGFR allele. 19. The method of claim 1, wherein the cancer is homozygous for wild-type activity of the EGFR protein. 20. The method of claim 1, wherein the activity of the wild-type EGFR protein is overexpressed or upregulated. 21. The method of claim 1, wherein the expressed EGFR protein has a wild-type active site. 22. The method of claim 21, wherein the cancer is characterized by at least one copy of Exon 19 of the EGFR gene. 23. The method of claim 1, wherein the compound is administered in a dose of about 32 mg/m.sup.2. 24. The method of claim 1, wherein the compound is administered in a dose of about 20 mg/m.sup.2.

Details for Patent 10,507,210

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Eli Lilly And Company	ERBITUX	cetuximab	Injection	125084	02/12/2004		2034-12-03
Eli Lilly And Company	ERBITUX	cetuximab	Injection	125084	03/28/2007		2034-12-03