NIRSUM LABORATORIES, INC.

7TUC8

Active

Non-Manufacturer

2025-02-25

2030-02-25

2026-02-22

NIKEJ SHAH

2024-08-29

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Department of Health and Human Services

SELECT LATE-STAGE CMC, NON-CLINICAL STUDIES, AND QUALITY PROGRAMS TO ACCELERATE NRS-033 TOWARDS PIVOTAL STUDIES AND REGISTRATION IN OPIOID USE DISORDER - PROJECT SUMMARY THE EPIDEMIC OF OPIOID USE DISORDER (OUD) IS THE GREATEST PUBLIC HEALTH CRISIS THE UNITED STATES HAS FACED IN A GENERATION. YET ESSENTIALLY THE SAME THREE FOOD AND DRUG ADMINISTRATION (FDA) APPROVED MEDICATIONS FOR OUD (MOUD), IN VARIOUS FORMULATIONS, HAVE BEEN AVAILABLE SINCE THE CRISIS BEGAN DECADES AGO: OPIOID AGONIST METHADONE, PARTIAL AGONIST BUPRENORPHINE AND ANTAGONIST NALTREXONE. THESE FEW LEGACY DEFENSES AGAINST THE STAGGERING TIDE OF ADDICTION HAVE PROVEN FEEBLE, PRIMARILY DUE TO SHORT TREATMENT RETENTION AND LACK OF ACCESS. THESE MOUD ARE POORLY ACCEPTED, OFFERED TO <20% OF INDICATED PATIENTS. IN THE SIGNIFICANT SUB-POPULATION OF OUD PATIENTS SEEKING OPIOID ABSTINENCE, ONLY ONE MOUD, MONTHLY INJECTABLE EXTENDED-RELEASE NALTREXONE (XR-NTX) IS INDICATED. HOWEVER, THE MEDIAN TREATMENT DURATION ON XR-NTX IS JUST ~30 DAYS (I.E., A SINGLE INITIAL INJECTION). FURTHER, GIVEN ITS HIGHLY VARIABLE PHARMACOKINETICS (PK), XR-NTX APPEARS TO LOSE EFFICACY IN A SUBSTANTIAL GROUP OF PATIENTS IN THE FOURTH WEEK PRIOR TO REPEAT DOSING, WITH ABRUPT LOSS OF ALL OPIOID BLOCKADE IN MOST PATIENTS WITHIN A WEEK AFTER A MISSED DOSE, LEAVING OPIOID INTOLERANT PATIENTS COMPLETELY UNPROTECTED. XR- NTX’S REFRIGERATION, TIME-CONSUMING 30-MINUTE THAWING, AND CUMBERSOME RECONSTITUTION REQUIREMENTS CREATE WORKFLOW FRICTION AND STORAGE CHALLENGES IN MANY ADDICTION PRACTICE SETTINGS, HINDERING AVAILABILITY. AS A RESULT, EVEN AFTER SUCCESSFUL MEDICAL WITHDRAWAL (I.E., OPIOID DETOXIFICATION), AN ESTIMATED ~95% OF ABSTINENCE-SEEKING PATIENTS ARE DISCHARGED UN-INITIATED ONTO XR-NTX, RESULTING IN RELAPSE RATES OF UP TO 90% WITHIN A YEAR. NRS- 033 IS A PATENTED NOVEL CHEMICAL COMPOSITION ULTRA LONG-ACTING OPIOID ANTAGONIST WITH SUCCESSFUL PRELIMINARY PHASE 1 CLINICAL DATA. THESE DATA SUGGEST NRS-033 WILL BE LONGER DURATION, STRONGER ACTING, MORE CONSISTENTLY EFFICACIOUS, AND MORE FORGIVINGLY DOSED THAN XR-NTX. NRS-033’S HUMAN PHASE 1 PK DATA SUGGESTS >400% LONGER DURATION OF ACTION THAN XR-NTX, CORRESPONDING TO DRAMATICALLY IMPROVED TREATMENT RETENTION. GIVEN ITS GRADUAL DECLINE AND HIGH TROUGH LEVELS OF PLASMA NALMEFENE, NRS-033 SHOULD PROVIDE STRONGER AND MORE CONSISTENT OPIOID BLOCKADE, AS WELL AS A MORE FORGIVING DOSING SCHEDULE THAN XR-NTX. SUCH UPGRADES ARE CRITICAL FOR SOCIALLY COMPLEX PATIENTS IN TODAY’S ILLICIT MARKET DOMINATED BY POTENT SYNTHETIC OPIOIDS, DIFFERENT FROM THAT DECADES AGO. ALSO, NRS-033 IS A ROOM TEMPERATURE STABLE READY-TO-USE PREFILLED SYRINGE, MUCH EASIER TO USE AND CLINICALLY ACCESSIBLE THAN XR-NTX. OUR PROPOSED AIMS SEEK TO EXPEDITE NRS-033 INTO PHASE 3 TRIALS AND FDA REGISTRATION, HENCE INCLUDE: LATE STAGE (REGISTRATION BATCH) CHEMISTRY, MANUFACTURING, AND CONTROLS (CMC) FOR API AND DRUG PRODUCT, REGISTRATION ENABLING NON-CLINICAL STUDIES, QUALITY SYSTEMS, AND REGULATORY ENGAGEMENT WITH FDA. DESPITE SIGNIFICANTLY DE-RISKED DEVELOPMENT, THE TIMELY ADVANCE OF NRS-033 WILL HAVE A PROFOUND PUBLIC HEALTH IMPACT ONCE AVAILABLE, REDUCING RELAPSE AND OVERDOSE RISK FOR ABSTINENCE-SEEKING OUD PATIENTS, HELPING DEFEAT THE PREVAILING STIGMA THAT OPIOID DEPENDENCE IS INESCAPABLE.

4785001.00

0.00

0.00

2022-09-15

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Department of Health and Human Services

DEVELOPMENT OF A NOVEL DRUG FOR TREATING OPIOID USE DISORDER - PROJECT SUMMARY THE ONGOING EPIDEMIC OF OPIOID USE DISORDER (OUD), OVERDOSE, AND DEATH IS UNPRECEDENTED. AVAILABLE PHARMACOLOGIC THERAPIES FOR OUD HAVE FAILED TO STEM THE TIDE, PLAGUED BY POOR ADHERENCE AND RETENTION, THE PRINCIPAL FACTORS ASSOCIATED WITH RELAPSE AND TREATMENT FAILURE. OVER 80% OF INDIVIDUALS WITH OUD ARE UNTREATED. MORE TREATMENT OPTIONS ARE NEEDED. THIS PROPOSAL SEEKS TO DEVELOP AN OUD PHARMACOLOGIC OPTION SUPERIOR TO CURRENTLY AVAILABLE THERAPIES. AGONIST/ PARTIAL AGONIST TREATMENTS WITH METHADONE AND BUPRENORPHINE CURRENTLY DOMINATE PHARMACOLOGIC THERAPIES FOR OUD. HOWEVER, ANTAGONIST THERAPY MAY BE MORE APPROPRIATE FOR IMPORTANT SUB-POPULATIONS: THE YOUNG, NEWLY ADDICTED, MILITARY, SELECT CRIMINAL JUSTICE CLIENTS, AND PATIENTS WHOSE EMPLOYMENT, BELIEFS, OR PREFERENCES MOTIVATE ABSTINENCE. ONCE-MONTHLY INJECTABLE EXTENDED-RELEASE NALTREXONE (XRN) RECEIVED FDA APPROVAL IN 2010 FOR TREATING OUD. DUE TO IMPROVED PATIENT ADHERENCE AND RETENTION RELATIVE TO ORAL ONCE-DAILY NALTREXONE, XRN IS GAINING WIDER ACCEPTANCE. US PRESCRIPTION VOLUME HAS GROWN ~37% IN 2017. STILL, EARLY PATIENT DISCONTINUATION WITH XRN IS PERVASIVE, AS WITH OTHER OUD TREATMENTS, OFTEN AFTER JUST 1 MONTH, USUALLY LEADING TO EARLY RELAPSE AND TREATMENT FAILURE. WE AIM TO MAINTAIN EFFECTIVE OPIOID ANTAGONISM WITH A SINGLE INJECTION LASTING AT LEAST TWO MONTHS, AND UP TO 4 MONTHS OR MORE, IMPROVING UPON THE ADHERENCE, RETENTION, AND TREATMENT BURDEN OF COMPARABLE THERAPIES. WE HAVE SYNTHESIZED A SERIES OF NOVEL AND PROPRIETARY SMALL MOLECULE ESTER-TYPE PRODRUGS OF FDA APPROVED OPIOID ANTAGONISTS, WITH ESTABLISHED PK/PD CORRELATIONS AND ANIMAL-HUMAN TRANSLATABILITY. THESE CANDIDATES ARE DESIGNED TO MEET FDA’S ABBREVIATED 505(B)2 APPROVAL PATH, REDUCING DEVELOPMENT AND REGULATORY RISK. BROAD PROVISIONAL PATENT PROTECTION IS FILED. OUR LEAD CANDIDATE, NRS-033, SHOWS IN VIVO CALCULATED T1/2 OF ~33 DAYS IN RATS FOR THE ACTIVE METABOLITE. PK MODELLING SUGGEST EVERY 3 MONTHS OR LONGER DOSING IS LIKELY IN HUMANS. NRS-033’S MEAN PLASMA CONCENTRATION OF ACTIVE METABOLITE AT 28 DAYS IS 2.15 NG/ML, WITH ABILITY TO DOSE >50% HIGHER, VS. XRN ~1.7 NG/ML, POSSIBLY ALLOWING STRONGER ANTAGONISM AGAINST POTENT SYNTHETIC OPIOIDS. FOR WOMEN WHO ARE PREGNANT AND OF CHILD-BEARING POTENTIAL, WE EXPECT MORE FAVORABLE PREGNANCY CATEGORY B FOR NRS-033, RATHER THAN C AS FOR ALL OTHER MAT. OUR UG3 AIMS INCLUDE: 1) LEAD CONFIRMATION STUDIES, LEAD SELECTION, FDA FAST TRACK FILING, AND TOXICOLOGY BATCH MANUFACTURING; 2) IND-ENABLING STUDIES, GMP MANUFACTURING, AND IND SUBMISSION; UH3 AIMS ARE, 3) PHASE 1 STUDIES, CARCINOGENICITY STUDIES, PHASE 2 CLINICAL TRIAL INITIATION, AND FDA BREAKTHROUGH THERAPY FILING. THE GOAL IS TO URGENTLY ADVANCE TO PHASE 3 TRIALS AND FDA APPROVAL. WE HYPOTHESIZE WE CAN DEVELOP A NOVEL THERAPEUTIC WITH SUPERIOR ADHERENCE AND RETENTION, THAT MAY BE BETTER INDICATED IN MANY WOMEN AND STRONGER VS. SYNTHETIC OPIOIDS. DESPITE ATYPICALLY LOWER DEVELOPMENT RISK, THIS TIMELY ADVANCE SHOULD HAVE A SIGNIFICANT PUBLIC HEALTH IMPACT BY REDUCING RATES OF RELAPSE, OVERDOSE, AND DEATH. CONFIDENTIAL

9160866.00

0.00

0.00

2020-05-02

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Small Business Administration

TO AID SMALL BUSINESSES IN MAINTAINING WORK FORCE DURING COVID-19 PANDEMIC.

0.00

48350.00

48350.00

2019-04-25

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Department of Health and Human Services

DEVELOPMENT OF A NOVEL DRUG FOR TREATING OPIOID USE DISORDER

6283350.00

0.00

0.00

2020-05-01

Paid in Full

100

48350

48350

Unanswered

Unknown/NotStated

Unanswered

Unanswered

48846.21