Non-immunosuppressive FK506 analogs and use thereof

Case ID:

C15634

Disclosure Date:

12/23/2018

Unmet Need
Chronic, nonhealing wounds are estimated to affect approximately 2% of the general population, and the cost of caring for these wounds exceeds $50 billion per year. These costs are expected to rise due to the increasing prevalence of diabetes and other diseases that hinder wound healing. Chronic infections increase morbidity and mortality in affected individuals and reduce quality of life. Consequently, novel therapeutics that accelerate wound healing are needed.

Technology Overview
The inventors have previously demonstrated that combination therapy with two drugs, FK506 and AMD3100, synergistically enhances wound healing in a diabetic mouse model. FK506 contributes to wound healing by activating BMP signaling through its binding and inhibition of FKB12. However, FK506 is a potent immunosuppressant with off target effects. To overcome this limitation, the inventors designed and synthesized a series of FK506 analogs that are not immunosuppressive. Importantly, these inhibitors retained their ability to bind FKB12 and activate BMP signaling. The inventors tested the FK506 analogs in combination with AMD3100 and observed the same acceleration of wound healing that was observed with FK506.

Stage of Development
The inventors synthesized FK506 analogs and confirmed their ability to synergize with AMD3100 to accelerate wound healing in a diabetic mouse model.

Patent Information:

Title	App Type	Country	Serial No.	Patent No.	File Date	Issued Date	Expire Date	Patent Status
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	Israel	285085		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	Canada	3,127,613		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	Australia	2020211994		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	Mexico	MX/A/2021/008824	413272	1/23/2020	5/21/2024	1/23/2040	Granted
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	South Africa	2021/05759		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	Korea (South)	10-2021-7026390		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	European Patent Office	20746065.0		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	China	2020800221718		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	Japan	2021-543343		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	India	202117035679		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	Hong Kong	62022053073.2		1/23/2020			Pending
NON-IMMUNOSUPPRESSIVE FK506 ANALOGS AND USE THEREOF	PCT: Patent Cooperation Treaty	United States	17/424,441		7/20/2021			Pending

Direct Link:

https://jhu.technologypublisher.com/technology/35368

Inventors:

Category(s):

Clinical and Disease Specializations > Wound Healing, Technology Classifications > Therapeutic Modalities > Small Molecules,

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For Information, Contact:

Vera Sampels

vsampel2@jhu.edu

410-614-0300

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