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Development of a Potent and Selective Nav1.8 inhibitor for the Treatment of Acute and Chronic Pain with the Goal of Reducing Opioid Use and Preventing Opioid Use Disorders

Award Number: UG3DA058552
ORGANIZATION: NATIONAL INSTITUTE ON DRUG ABUSE
OPDIV: NIH
AWARD CLASS: COOPERATIVE AGREEMENT
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 05/15/2023
PERIOD OF PERFORMANCE END DATE: 04/30/2025

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Development of a Potent and Selective Nav1.8 inhibitor for the Treatment of Acute and Chronic Pain with the Goal of Reducing Opioid Use and Preventing Opioid Use Disorders - PROJECT SUMMARY Voltage-gated sodium ion channels (NaVs) are required for the transmission of electrical signals along pain sensing neurons. While a number of NaV isoforms are expressed in nociceptors, NaV1.8 is unique in that its distribution is highly restricted to dorsal root ganglia and trigeminal neurons, raising the intriguing possibility that isoform selective inhibitors could interfere with pain signaling without affecting other physiological functions. In support of this hypothesis, rodents treated with antisense oligonucleotides targeting NaV1.8 exhibit reduced mechanical allodynia in models of inflammatory and neuropathic pain. Recently, Vertex has demonstrated that NaV1.8 inhibitors effectively reduce pain in patients with small fiber neuropathy, osteoarthritis and following surgery (bunionectomy, abdominoplasty). Despite these promising results, due to molecule-specific challenges such as poor pharmacokinetics, accumulation of metabolites, idiosyncratic drug reactions and high cost of goods, no drug candidate targeting NaV1.8 has yet reached approval. SiteOne Therapeutics has identified a development candidate targeting NaV1.8 with exquisite potency (IC50 < 1 nM at hNaV1.8), selectivity over off-target NaV isoforms (>8000-fold), and pharmaceutical properties suitable for once daily oral dosing. The objective of this proposal is to advance the development candidate through a single and multiple ascending dose study in healthy volunteers (UG3 phase), and Phase 2 proof-of-concept studies in acute postsurgical and chronic neuropathic pain (UH3 phase). If successful, the program will deliver an oral analgesic medicine targeting NaV1.8 for the treatment of pain and replacement of opioids that is well- positioned to initiate pivotal Phase 3 trials.


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: 2025 ( Subtotal = $0 )
2025	2023	SITEONE THERAPEUTICS, INC.	280 UTAH AVE STE 250	SOUTH SAN FRANCISCO	CA	94080	SAN MATEO	USA	Drug Use and Addiction Research Programs	000	1	9/10/2025	NEW	$0
														Subtotal = $0

Issue Date FY: 2024 ( Subtotal = $0 )
2024	2023	SITEONE THERAPEUTICS, INC.	280 UTAH AVE	SOUTH SAN FRANCISCO	CA	94080	SAN MATEO	USA	Drug Use and Addiction Research Programs	000	1	10/13/2023	NEW	$0
2024	2023	SITEONE THERAPEUTICS, INC.	280 UTAH AVE STE 250	SOUTH SAN FRANCISCO	CA	94080	SAN MATEO	USA	Drug Use and Addiction Research Programs	001	1	8/5/2024	NEW	$0
														Subtotal = $0

Issue Date FY: 2023 ( Subtotal = $5,341,667 )
2023	2023	SITEONE THERAPEUTICS, INC.	280 UTAH AVE	SOUTH SAN FRANCISCO	CA	94080	SAN MATEO	USA	Drug Use and Addiction Research Programs	000	1	5/4/2023	NEW	$5,341,667
														Subtotal = $5,341,667

Grand Total All Awards = $5,341,667

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Development of a Potent and Selective Nav1.8 inhibitor for the Treatment of Acute and Chronic Pain with the Goal of Reducing Opioid Use and Preventing Opioid Use Disorders

Award Number: UG3DA058552

ORGANIZATION: NATIONAL INSTITUTE ON DRUG ABUSE

OPDIV: NIH

AWARD CLASS: COOPERATIVE AGREEMENT

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

PERIOD OF PERFORMANCE START DATE: 05/15/2023

PERIOD OF PERFORMANCE END DATE: 04/30/2025

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