HSPC-sparing treatments for Rb-positive abnormal cellular proliferation

Patent metadata

Field	Value
Publication number	US-10434104-B2
Application number	US-201816112362-A
Country	US
Kind code	B2
Filing date	Aug 24, 2018
Priority date	Mar 15, 2013
Publication date	Oct 8, 2019
Grant date	Oct 8, 2019

Abstract

This invention is in the area of improved compounds for and methods of treating selected RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, improved treatment of select RB-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as highly selective and, in certain embodiments, short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.

First claim

We claim:

1. A method of treating a human with estrogen-receptor positive breast cancer comprising administering to the human an effective amount of a selective cyclin dependent kinase 4/6 (CDK4/6) inhibitor of the formula:

and
administering to the human an effective amount of goserelin.

2. The method of claim 1 , wherein the estrogen-receptor positive breast cancer is HER2-negative.

3. The method of claim 1 , wherein the CDK4/6 inhibitor is administered orally.

4. The method of claim 1 , wherein the CDK4/6 inhibitor is administered at least once a day for 28 or more continuous days.

5. The method of claim 4 , wherein the CDK4/6 inhibitor is administered twice a day.

6. A method of treating a human with estrogen-receptor positive breast cancer comprising administering to the human an effective amount of a selective cyclin dependent kinase 4/6 (CDK4/6) inhibitor of the formula:

wherein the CDK4/6 inhibitor is administered in a therapeutic regime with goserelin.

7. The method of claim 6 , wherein the estrogen-receptor positive breast cancer is HER2 negative.

8. The method of claim 6 , wherein the CDK4/6 inhibitor is administered orally.

9. The method of claim 5 , wherein the CDK4/6 inhibitor is administered at least once a day for 28 or more continuous days.

10. The method of claim 9 , wherein the CDK4/6 inhibitor is administered twice a day.

Assignees

• G1 Therapeutics Inc

Inventors

• Strum Jay Copeland
• Bisi John Emerson
• Roberts Patrick Joseph
• Tavares Francis Xavier

Classifications

• A61K2300/00

  Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00 · CPC title

• A61P35/04

  specific for metastasis · CPC title

• A61K31/7048

  having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin {, digitoxin or digoxin} · CPC title

• A61K31/555

  containing heavy metals, e.g. hemin, hematin, melarsoprol · CPC title

• A61K31/527 Primary

  spiro-condensed · CPC title