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buprenorphine (Transtec Pro / Transtec)

✓ Approved

Napp Pharmaceuticals · OPRK1 · 小分子

什么是 buprenorphine？

buprenorphine 是一种小分子，由Napp Pharmaceuticals研发。该药已获批，用于治疗相关适应症，给药途径：Topical。

药物档案

商品名Transtec Pro, Transtec
公司Napp Pharmaceuticals
药物类别小分子
分子靶点OPRK1, OPRM1
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Napp Pharmaceuticals

作用机制

分子靶点

buprenorphine 作用于 2 个分子靶点：

OPRK1opioid receptor kappa 1 (KOR1, OPRK)
OPRM1opioid receptor mu 1 (MOR1, LMOR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

buprenorphine 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Cancer pain✓ Approved

相关研究文献

PubMedAdvances in therapy2026-09-10

Brixadi for Stimulant Use Disorder: Evolving Pharmacologic Considerations and Clinical Implications.

Sawaya M Farris MF, McNulty Molly E ME, Germain Collin J St CJS, Hachem Ibraheem A IA et al.

Substance use disorders are an increasing concern globally, causing a tremendous uptick in public health burden in recent years. Despite the growing attention these disorders receive, there remain no approved pharmacotherapies for stimulant use disorder, thereby contributing a major portion of this burden. This review examines the potential use of Brixadi, an extended-release injectable formulation of the widely used pharmacotherapy buprenorphine, indicated for opioid use disorder, in the treatment of stimulant use disorder. Psychostimulants, including cocaine, methamphetamine, and designer stimulants, all exert their effects by inhibiting or reversing the directionality of the monoamine transporters in the synaptic cleft. Inhibition or reversal of these transporters in the synaptic cleft allows dopamine, serotonin, and norepinephrine to remain in the synapse, which ultimately enhances their activity and contributes to the reinforcement of substance use. The reinforcement loop driven by excess neurotransmitters, particularly dopamine, provides a pharmacotherapeutic target via receptor interactions. Brixadi is an injectable extended-release buprenorphine primarily used to treat opioid use disorder. The extended-release mechanism enables sustained drug-receptor interaction, resulting in stable plasma drug concentrations. Buprenorphine is as a dual-acting agent, a partial μ-opioid receptor (MOR) agonist and a κ-opioid receptor (KOR) antagonist. KOR antagonism modulates symptoms of withdrawal in OUD, including dysphoria, stress, and drug cravings. Therefore, Brixadi's KOR antagonism may offer a promising pharmacologic target for stimulant use disorder recovery by mitigating these negative affective states. Additionally, the bimodal mechanism suggests that Brixadi may be a beneficial pharmacologic candidate for people who suffer from polysubstance use involving opioids and psychostimulants. While there is promise behind these developments, current studies are limited to preclinical trials and have not yet advanced toward clinical trials. However, Brixadi's extended-release profile and potential capability to minimize withdrawal-related dysphoria and stress-induced drug seeking present promise for further clinical investigation.

PMID 42720725
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PubMedJournal of addiction medicine2026-09-08

Treatment Discontinuation and Barriers and Facilitators to Retention Among Individuals Initiating Buprenorphine for Opioid Use Disorder: A Longitudinal Cohort Study.

Poulsen Melissa N MN, Truong Michelle L ML, Pabla Jasmine K JK, Poissant Amy A et al.

Early discontinuation of medication for opioid use disorder (MOUD) is associated with increased mortality and hinders remission. Combining data from electronic health records (EHRs) and patient questionnaires, we examined buprenorphine discontinuation and barriers and facilitators to retention in outpatient settings. Adults initiating buprenorphine in a Pennsylvania outpatient program (2021-2023) completed 2 questionnaires: at medication initiation (baseline) and 6 months after initiation (follow-up). Among 1189 eligible patients, we evaluated buprenorphine discontinuation (≥30-d gap in medication supply) and compared demographic factors using EHRs. We identified discontinuation reasons among survey participants (baseline n = 374; follow-up n = 197) through medical record review; questionnaires assessed treatment barriers and facilitators. Within 6 months, 629 (53%) patients discontinued buprenorphine, though 15% restarted medication within the 6-month period. Discontinuation was more common among younger patients. Among baseline survey participants, discontinuation was usually unplanned (66%) or against provider advice (19%). Among follow-up participants who discontinued the program during the follow-up period, 54% reported receiving MOUD at 6 months, indicating that many transition to other treatment programs. Those not receiving medication at 6 months cited lack of need (46%). Travel challenges (distance/transportation to clinics), scheduling, and mental health conditions were common barriers to treatment; facilitators centered on improving these factors and clinic processes. Observed patterns reflect dynamic and noncontinuous receipt of medication over time and underscore the early months of treatment as a critical window for supporting buprenorphine engagement. Findings reveal actionable areas to improve retention by reducing logistical burdens, enhancing nonjudgmental therapeutic support, and integrating mental health care.

PMID 42709580
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PubMedCureus2026-09-07

When Tapering Is Not an Option: Transitioning From High-Dose Methadone to Buprenorphine.

Petelinsek Sarah S, Morris Jarom J, Zaugg Ethan E, Coudreaut Michael M

Methadone is a commonly used medication for opioid use disorder (OUD) but carries known risks, including corrected QT interval (QTc) prolongation and ventricular arrhythmias. Current guidelines recommend gradual methadone tapering or buprenorphine microdosing when transitioning to buprenorphine to minimize precipitated withdrawal. However, evidence guiding management when methadone must be urgently discontinued because of medical contraindications is limited. We describe a 41-year-old woman with OUD receiving high-dose methadone who presented after cardiac arrest with marked QTc prolongation, hypokalemia, and suspected methadone-associated cardiotoxicity. Given the life-threatening risk of ventricular arrhythmias, methadone was discontinued without tapering. The patient was managed symptomatically with short-acting opioids for withdrawal and was subsequently initiated on buprenorphine approximately 60 hours after her last methadone dose, once moderate withdrawal had developed. Although she experienced transient worsening of withdrawal symptoms after induction, she stabilized within 48 hours and was discharged on maintenance buprenorphine with outpatient follow-up. While gradual tapering remains standard practice, this case demonstrates that complete methadone cessation without tapering, followed by appropriately timed buprenorphine initiation, may be feasible when rapid discontinuation is medically necessary. Careful monitoring, shared decision-making, and symptomatic support remain essential.

PMID 42703179
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PubMedAddictive behaviors2026-09-07

Facility, community, and state-level correlates of overdose education and naloxone provision in substance use treatment facilities in the United States.

Cano Manuel M, Green Traci C TC

This study examined which characteristics of substance use disorder (SUD) treatment facilities and their surrounding areas are associated with offering overdose education and naloxone (OEN). We linked data from eight national sources regarding 12,146 SUD treatment facilities (from the 2024 National Directory of Drug and Alcohol Use Treatment Facilities) and the communities and states where they operate. Regression analyses tested whether facility OEN provision was associated with facility type (with cluster analysis used to group facilities based on services offered) and selected facility, ZIP code, and state characteristics. In a generalized linear mixed model, odds of OEN provision were higher in facilities that: used medications for opioid use disorder (Adjusted Odds Ratio [AOR] 7.21; 95% Confidence Interval [CI] 5.97-8.71); offered testing for HIV/hepatitis (AOR 2.39; 95% CI, 2.00-2.86); were government-operated (AOR 2.37; 95% CI, 1.81-3.11) vs. private for-profit; accepted Medicaid (AOR 2.36; 95% CI, 2.01-2.77); or were in metropolitan (vs. non-metropolitan) areas (AOR 1.27; 95% CI, 1.06-1.53). In facility cluster analysis (based on 191 facility characteristics/services), adjusted odds of OEN provision were lowest in the cluster characterized by outpatient services, low use of medications for opioid use disorder, and few social/medical/tailored services. Odds of OEN provision were highest in the cluster characterized by offering "detoxification," residential care, buprenorphine and naltrexone, and comprehensive medical and social services. OEN provision is lowest in SUD treatment facilities that do not use medications for opioid use disorder, offer relatively few social or medical services, and/or are located in non-metropolitan areas.

PMID 42705149
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PubMedDrug and alcohol dependence reports2026-09-06

Discontinuing extended-release buprenorphine: Participant experiences from a mixed-methods observational study.

Fishman Marc M, Stoops William W, Podesta Arwen A, Wyatt Stephen A SA et al.

Although clinical guidelines support long-term buprenorphine treatment for opioid use disorder (OUD), evidence guiding planned discontinuation is limited. Extended-release buprenorphine (BUP-XR) produces a slow decline in plasma concentrations that may function as a natural taper. This study examined clinical and qualitative outcomes following planned BUP-XR discontinuation. This observational study followed participants for 6 months after BUP-XR discontinuation and included qualitative interviews exploring perspectives on discontinuation. Eligibility: adults with ≥ 12 months BUP-XR treatment, controlled OUD and other substances, and joint provider-participant agreement on treatment discontinuation. Primary endpoint: successful treatment discontinuation at 6 months, defined as no consistent self-reported nonmedical opioid use (≥1 day/week for 4 consecutive weeks or 7 consecutive days) and not restarting long-term OUD treatment due to withdrawal symptoms or nonmedical opioid use. Twelve participants enrolled; one excluded for ineligibility. Eleven completed 6-month follow-up; 10/11(90.1%) met successful discontinuation criteria. Withdrawal symptoms were generally mild, nonpersistent, and resolved by Month 6. Opioid craving remained low throughout. No deaths, pregnancies, overdoses, or withdrawal-related adverse events occurred. One participant experienced non-study-related adverse events: pneumonia/empyema with hospitalization and macrocytic anemia. At interviews (on average 12 months post-discontinuation), all participants remained off treatment without persistent opioid use; one reported a brief, time-limited return to opioid use. Participants described minimal opioid withdrawal, low craving, and stable functioning across domains. After long-term BUP-XR treatment, discontinuation was effective and well tolerated over 6 months. BUP-XR's pharmacokinetic profile may safely support a gradual taper when paired with patient-centered care, psychosocial support, and ongoing engagement.

PMID 42699707
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PubMedJournal of addiction medicine2026-09-04

Opioid Use Disorder Outcomes Following Inpatient Opioid Withdrawal Management.

Bailey Genie L GL, Lee Joshua D JD, Nunes Edward V EV, Tofighi Babak B et al.

Medically assisted withdrawal (MAW) for opioid use disorders (OUD) remains common. NIDA's CTN-0051 (X:BOT) trial compared two OUD medications initiated during an acute inpatient MAW admission and continued postdischarge at 8 US sites. This ancillary observational follow-on study explored treatment-as-usual outcomes at 5 X:BOT sites. Adults admitted for OUD were conveniently and consecutively recruited to an 8-week, prospective, observational, noninterventional study targeting up to 300 participants. Withdrawal protocols and medications for OUD (MOUD) followed site usual practices. Baseline and postdischarge weeks 1, 4, and 8 measures were OUD severity, length-of-stay (LOS), urine samples, self-reported MOUD, nonprescribed opioid use, and overdoses. Data analyses were descriptive. A total of N = 211 enrolled participants were primarily white men (74%) with daily heroin (87.2%) and intravenous (64.0%) use. About 41.7% (n = 88) reported MOUD treatment at discharge: extended-release naltrexone (n = 39), sublingual buprenorphine-naloxone (n = 38), methadone (n = 8), and oral naltrexone (n = 3). Self-reported MOUD use at week 8 was 28.0%, when 52.6% reported no regular use (<7 consecutive days) and 25.6% reported nonprescribed opioid abstinence. Negative urine rates for nonprescribed opioids ranged from 26.1% to 31.3%. One overdose death and 17 nonfatal opioid-related overdose events occurred in 15 participants. Return to nonprescribed opioid use, frequent overdose events, one death, and a relative lack of MOUD treatment uptake characterized this usual care cohort following inpatient OUD admissions. These findings underscore the urgent need for individuals and providers to prioritize linkage to evidence-based MOUD treatments following acute inpatient OUD-related admissions, given high rates of return to opioid use and overdose events.

PMID 42696557
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