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Development of an oral analgesic with reduced liabilities

Award Number: R44DA056336
ORGANIZATION: NATIONAL INSTITUTE ON DRUG ABUSE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 04/15/2022
PERIOD OF PERFORMANCE END DATE: 03/31/2024

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Development of an oral analgesic with reduced liabilities - Abstract Oral mu-opioid receptor (MOR) agonists with high receptor level activity remain the primary treatment for pain (about 702 million oral opioid pain prescriptions are dispensed per year in the US). However, these compounds are addictive and have dangerous levels of respiratory depression. MOR agonists that are classified as “weaker” like buprenorphine and tramadol reduce these serious adverse events (SAE), but they retain many liabilities that keep them from displacing more addictive and dangerous compounds like oxycodone. Up to 25% of patients receiving opioid prescriptions are at risk of addiction or an SAE that requires medical care. Stemming this tide requires a better partial MOR agonist. Using a novel MOR-ligand scaffold, Epiodyne has developed a promising series of potent orally bioavailable drug-like small molecules. From this series, our development candidate EPD2520 was selected; EPD2520 is a MOR partial agonist, that exhibits analgesic efficacy comparable to non-lethal doses of oxycodone, with little to no respiratory depression, and with apparently less abuse liability in rats than buprenorphine. In addition to a promising behavioral profile, EPD2520 also appears to be suitable for chronic administration. Safety issues were not detected in in-vitro screens including receptor selectivity, carcinogenicity, QT prolongation, metabolism ID and CYP inhibition assays. In this project we will 1) advance EPD2520 to IND enabling studies and file an IND. And 2) investigate novel ligand-receptor-physiology interactions to design 2nd generation compounds that build on the efficacy, drug like properties and reduced liabilities of EPD2520. We anticipate that EPD2520 will be a highly efficacious analgesic with reduced respiratory and addiction liabilities.


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: 2023 ( Subtotal = $1,488,866 )
2023	2023	EPIODYNE INC	953 INDIANA ST	SAN FRANCISCO	CA	94107	SAN FRANCISCO	USA	Drug Use and Addiction Research Programs	000	2	3/29/2023	NON-COMPETING CONTINUATION	$1,488,866
														Subtotal = $1,488,866

Issue Date FY: 2022 ( Subtotal = $1,011,134 )
2022	2022	EPIODYNE, INC.	953 INDIANA ST	SAN FRANCISCO	CA	94107	SAN FRANCISCO	USA	Drug Use and Addiction Research Programs	000	1	4/6/2022	NEW	$1,011,134
														Subtotal = $1,011,134

Grand Total All Awards = $2,500,000

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Development of an oral analgesic with reduced liabilities

Award Number: R44DA056336

ORGANIZATION: NATIONAL INSTITUTE ON DRUG ABUSE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

PERIOD OF PERFORMANCE START DATE: 04/15/2022

PERIOD OF PERFORMANCE END DATE: 03/31/2024

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