Napp Pharmaceuticals · OPRK1 · 小分子
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。
| 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 |
buprenorphine 作用于 2 个分子靶点：
| OPRK1 | opioid receptor kappa 1 (KOR1, OPRK) |
| OPRM1 | opioid receptor mu 1 (MOR1, LMOR) |
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 disorders | Abdominal pain | ✓ Approved |
| Neoplasms benign, malignant and unspecified (incl cysts and polyps) | Cancer pain | ✓ Approved |
Chukwudi Kelechi Nnaemeka KN, Adediji Godwin G, Lynch Meghan M, Scully Michael M et al.
Maguire Lindsay A LA, Jha Manish K MK, Murphy Nicholas N, Thomas Ynhi T YT
Wong Aaron K AK, McManus Helen H, Vogrin Sara S, Dib Youseph Y et al.
Ongoing disruptions to opioid supply in Australia have raised ongoing concerns about their impact on cancer pain management. The withdrawal of hydromorphone slow-release (SR) tablets from the Australian market has presented challenges to advanced cancer pain management. This study aimed to determine how this affected the utilisation of alternative slow-release opioids in patients with advanced cancer. A retrospective cohort study was conducted at a quaternary cancer centre, comparing opioid prescribing patterns across two 12-month periods: before hydromorphone SR tablet discontinuation was announced and after its discontinuation. Inpatient and outpatient prescribing data were analysed for adult patients with incurable advanced or metastatic cancer who first presented to the centre during each study period. A total of 2856 patients were included (n = 1475 pre and n = 1381 post hydromorphone SR discontinuation). Following hydromorphone SR withdrawal, opioid prescribing patterns shifted. Methadone use rose modestly (adjusted odds ratio [aOR] 1.42, p = 0.07), accompanied by a doubling of median dose (45 mg vs. 22.5 mg; p = 0.005). Morphine use declined (aOR 0.69, p < 0.001), yet daily OMEDD increased by ∼20% (95% confidence interval 1.01-1.37). Tapentadol (aOR 1.40, p = 0.01) and buprenorphine (aOR 1.37, p < 0.001) were prescribed more frequently, without corresponding dose escalation. Following hydromorphone SR withdrawal, the frequency of methadone use increased and median doses doubled. Research incorporating national datasets is needed to clarify the broader impact of opioid supply interruptions. These findings indicate a potential need to reframe the place of methadone in practice, and potentially upscale the focus of clinician training on its safe and effective use.
Evans Elizabeth A EA, Stopka Thomas J TJ, Pivovarova Ekaterina E, Ryan Danielle D et al.
Limited access to medications for opioid use disorder (MOUD) is a major driver of the opioid overdose crisis. Jails have been slow to implement MOUD treatment, especially agonist medications (methadone, buprenorphine). Massachusetts mandated certain county jails pilot-test delivery of all FDA-approved MOUD treatments, stipulating jails continue MOUD, or initiate it prior to release, and facilitate MOUD continuation in the community post-release. The Massachusetts Justice Community Opioid Innovation Network (MassJCOIN) partnered with seven pilot jails, the Massachusetts Department of Public Health, and community treatment providers to conduct a Type 1 hybrid effectiveness-implementation study of this carceral MOUD program. Drawing from selected MassJCOIN evidence on MOUD treatment program implementation, outcomes, and costs, we consider how findings can inform more effective, humane public health and clinical responses to treating incarcerated individuals. MOUD treatment in jail improves treatment engagement, reduces recidivism, and saves lives. MOUD program implementation facilitators included: policies and processes to offer universal MOUD access; transformative and adaptive leadership; appropriate staffing capacity and capabilities; proactive prevention of MOUD diversion; and consideration of patient preferences for MOUD treatment and co-occurring mental health conditions. MOUD program success was influenced by the legislative mandate and other major statewide changes and a community-based treatment system conducive to MOUD implementation. MOUD treatment continuity post-release was facilitated by re-entry planning and preparing individuals for post-release risk environments. Site-specific costs of implementing and sustaining MOUD programming provide information for decisions about program design, budgetary needs, and resource allocation. Carceral MOUD programming is a compelling strategy to advance public safety and public health. Lessons learned provide a playbook for broader diffusion of carceral MOUD programs and can help carceral leadership, healthcare providers, and policymakers make carceral healthcare improvements. Within a harm reduction framework, carceral MOUD treatment can provide substantial opportunities to fill gaps in public health prevention efforts and clinical care to reduce opioid overdose and other concomitant risks. Carceral MOUD programming offers ways for carceral systems to work for the common good, garner trust in public institutions, and increase their legitimacy and value as public institutions.
Nacev Erin C EC, Prewitt Kristin C KC, Peng Linda L, Song Eugene E et al.
To describe real-world use of long-acting injectable buprenorphine among pregnant individuals with opioid use disorder (OUD), including monthly formulations and initiation among those not previously stable on sublingual buprenorphine. We conducted a retrospective chart review of inpatient and outpatient medical records of pregnant individuals with OUD who received at least one dose of long-acting injectable buprenorphine during pregnancy while admitted at a large academic medical center. Dosing patterns, supplemental sublingual buprenorphine use, treatment retention, and maternal outcomes were described. Between January 1, 2024, and February 1, 2026, 12 pregnant individuals received long-acting injectable buprenorphine. Most received monthly formulations (11 of 12). Ten patients (83.3%) initiated treatment with long-acting injectable buprenorphine during pregnancy through low-dose buprenorphine initiation; two continued long-acting injectable buprenorphine that was started before pregnancy. Median gestational age for those who initiated long-acting injectable buprenorphine during pregnancy was 30 weeks (range 11-33 weeks). All patients newly initiated on long-acting injectable buprenorphine reported nonprescribed fentanyl use before treatment. Supplemental sublingual buprenorphine was prescribed for all participants initiating long-acting injectable buprenorphine (median 20 mg/d, range 12-32 mg/d). Four who initiated long-acting injectable buprenorphine transitioned to methadone during pregnancy because of persistent cravings or withdrawal. At delivery, retention on long-acting injectable buprenorphine was 66.7%, and 91.7% remained on any medication for OUD (MOUD). Among pregnant individuals who received long-acting injectable buprenorphine, including those with nonprescribed fentanyl use initiating treatment during pregnancy, retention on MOUD through delivery was high, and supplemental buprenorphine was commonly prescribed. Some patients transitioned to methadone, underscoring the importance of individualized treatment and counseling regarding formulation-specific considerations.
Jafari Saeede S, Rahimi-Movaghar Afarin A, Noroozi Alireza A, Malekifar Pooneh P et al.
Extended-release injectable naltrexone (XR-NTX), a long-acting opioid antagonist, is an effective relapse prevention strategy in the treatment of opioid use disorder (OUD). However, standard XR-NTX initiation requires completion of opioid withdrawal management and a 1-2 week opioid-free period. This interval is associated with heightened vulnerability to lapse and relapse, and many patients fail to initiate XR-NTX treatment successfully. Therefore, alternative strategies that enable rapid XR-NTX initiation are needed. This study aimed to compare the effectiveness and safety of naltrexone-accelerated (NA) versus sublingual buprenorphine (SB) withdrawal management in facilitating XR-NTX initiation among patients with OUD. This single-center, open-label, randomized controlled trial uses a parallel-group design. Eligible patients aged 18-60 years with moderate to severe OUD who are actively using opioids and are not receiving regular maintenance treatment with methadone or buprenorphine are randomly assigned to one of two groups: (1) NA withdrawal management, comprising one day of adjunctive non-opioid medications, one day of buprenorphine administration, one day of washout, and four days of gradual oral naltrexone titration (1, 3, 12, and 25 mg/day); or (2) SB withdrawal management, comprising one day of adjunctive non-opioid medications, six days of buprenorphine tapering (up to 8 mg on Day 2, 6 mg on Day 3, 4 mg on Days 4-5, 2 mg on Day 6, and 1 mg on Day 7), and a seven-day washout period. Adjunctive non-opioid medications in both groups comprised clonidine, clonazepam, gabapentin, and trazodone. The primary outcomes are the proportions of participants who (1) achieve a negative urine drug test for the assessed opioids and (2) receive XR-NTX at the end of the withdrawal management period. Secondary outcomes include severity of withdrawal symptoms, opioid craving intensity, and adverse effects. All analyses are conducted according to the intention-to-treat principle. The findings of this trial may provide clinically relevant evidence to support rapid initiation of XR-NTX treatment in patients with OUD and inform clinical practice. https://en.irct.ir/trial/81525, Iranian Registry of Clinical Trials IRCT20250123064499N1.
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