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Novel Orally-Active Plasma Kallikrein Inhibitors for Diabetic Retinopathy

Award Number: R44EY019629
ORGANIZATION: NATIONAL EYE INSTITUTE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 09/10/2007
PERIOD OF PERFORMANCE END DATE: 02/29/2016

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Novel Orally-Active Plasma Kallikrein Inhibitors for Diabetic Retinopathy - DESCRIPTION (provided by applicant): There are nearly 24 million people in the U.S. who suffer from diabetes and all are at risk for developing diabetic macular edema (DME), a vision-threatening retinal complication of diabetes that is the leading cause of blindness in working age adults. Current prevalence of DME in the U.S. is estimated to be between 1.2 - 2.1 million. Increased retinal vascular permeability (RVP) to plasma proteins and fluid, resulting from breakdown of the blood-retinal barrier, leads to a build-up of fluid in the central portion of the retina - the macula - and the development of DME. The serine protease plasma kallikrein (PK) has been recently implicated as a pathological mediator of increased RVP in diabetes. In work carried out in phase I and phase II, ActiveSite has developed novel potent and selective PK inhibitors that reduce pathological RVP induced in clinically relevant rodent models of hypertension and diabetes following systemic, non-ocular administration. Based on efficacy and safety studies carried out in phase II, a lead PK inhibitor has been identified that has been shown to be effective in lowering pathological RVP following daily oral dosing at a moderate daily dose level. Repeat-dose range-finding toxicology studies in rats with the lead compound resulted in dose- proportional drug exposure, and, importantly, did not result in detectable adverse effects on any parameter at the highest dose tested, a dose that resulted in daily exposure to the active compound >40-fold higher than that seen at the efficacious dose, predictive of a high therapeutic index in the clinic. Based on the efficacy and preliminary safety assessments, the specific aims of this competitive phase II renewal application are to carry out FDA-required safety and toxicology studies with the lead PK inhibitor, studies that once completed successfully, would allow for the compilation and filing of an IND application with the FDA for initiating first-in-human Phase I clinical trials for oral treatment for DME.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2015 ( Subtotal = $0 )
2015	2013	ACTIVESITE PHARMACEUTICALS INC	1456 FOURTH STREET	BERKELEY	CA	94710	ALAMEDA	USA	Vision Research	000	5	3/11/2015	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2013 ( Subtotal = $699,825 )
2013	2013	ACTIVESITE PHARMACEUTICALS INC	626 BANCROFT WAY	BERKELEY	CA	94710	ALAMEDA	USA	Vision Research	000	5	2/13/2013	NON-COMPETING CONTINUATION	$699,825
														Subtotal = $699,825

Issue Date FY: 2012 ( Subtotal = $660,118 )
2012	2012	ACTIVESITE PHARMACEUTICALS INC	626 BANCROFT WAY	BERKELEY	CA	94710	ALAMEDA	USA	Vision Research	000	4	2/13/2012	COMPETING CONTINUATION	$660,118
														Subtotal = $660,118

Issue Date FY: 2010 ( Subtotal = $389,453 )
2010	2010	ACTIVESITE PHARMACEUTICALS INC	626 BANCROFT WAY	BERKELEY	CA	94710	ALAMEDA	USA	Vision Research	000	3	6/14/2010	NON-COMPETING CONTINUATION	$389,453
														Subtotal = $389,453

Issue Date FY: 2009 ( Subtotal = $435,382 )
2009	2009	ACTIVESITE PHARMACEUTICALS INC	626 BANCROFT WAY	BERKELEY	CA	94710	ALAMEDA	USA	Vision Research	000	2	6/11/2009	CHANGE OF GRANTEE / TRAINING INSTITUTION / AWARDING INSTITUTION	$435,382
														Subtotal = $435,382

Grand Total All Awards = $2,184,778

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Novel Orally-Active Plasma Kallikrein Inhibitors for Diabetic Retinopathy

Award Number: R44EY019629

ORGANIZATION: NATIONAL EYE INSTITUTE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 09/10/2007

PERIOD OF PERFORMANCE END DATE: 02/29/2016

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