Drug Database
BU

buprenorphine (Transtec Pro / Transtec)

✓ Approved

Napp Pharmaceuticals · OPRK1 · Small Molecule

What is buprenorphine?

buprenorphine is a small molecule developed by Napp Pharmaceuticals. It is approved for therapeutic indications via topical.

Drug Profile

Brand NamesTranstec Pro, Transtec
CompanyNapp Pharmaceuticals
Drug ClassSmall Molecule
Molecular TargetOPRK1, OPRM1
RouteTopical
StatusApproved
Sources: ClinicalTrials.gov, Napp Pharmaceuticals

Mechanism of Action

Molecular Targets

buprenorphine acts on 2 molecular targets:

OPRK1opioid receptor kappa 1 (KOR1, OPRK)
OPRM1opioid receptor mu 1 (MOR1, LMOR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

buprenorphine is developed for 2 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Gastrointestinal disordersAbdominal pain✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Cancer pain✓ Approved

Related Research Articles

PubMedLaboratory animal research2026-08-25

Evaluation of a human slow-release buprenorphine formulation in rats - tactile sensitivity and plasma concentration.

Kazantzi Spyridoula S, Jensen Mette N MN, Haanes Kristian A KA, Nordahl Karin M L KML

Opioids are considered ideal for managing moderate to severe post-operative pain in laboratory rodents, with buprenorphine being one of the most commonly used analgesics in rats. A long-acting buprenorphine formulation would be highly beneficial to avoid frequent dosing of postoperative animals; however, buprenorphine depot formulations developed for animal use are not available in Europe. The purpose of the present study was therefore to evaluate the effects in rats of a long-acting subcutaneous depot injection with buprenorphine developed for humans (Buvidal). Buvidal was evaluated in male Sprague Dawley rats alongside conventional short-acting buprenorphine (Temgesic) delivered subcutaneously and orally, a non-opioid analgesic (carprofen), and controls (saline). All three buprenorphine formulations resulted in significantly reduced mechanical sensitivity when assessed in pain-free, naïve rats using the von Frey pressure test at early time points (3-6 h), whereas carprofen and saline had no effect on tactile sensitivity. In a hypersensitivity model of cephalic allodynia, the hypoalgesic effect of Buvidal lasted beyond 24 h. Plasma concentrations support prolonged drug exposure following administration of the long-acting formulation, and levels exceeding 1 ng/mL were observed during periods of reduced tactile sensitivity. No significant effect on locomotor activity was found in an open field test following buprenorphine administration. Transient pica-like chewing behaviour and reduced alertness were observed in some buprenorphine-treated animals during the first hours after drug administration. The human slow-release buprenorphine formulation Buvidal produced sustained systemic exposure and prolonged hypoalgesic effects in male rats, as demonstrated in the cephalic hypersensitivity model, consistent with depot release kinetics. These results show that Buvidal is pharmacologically active in rats and may represent a potential approach for achieving sustained buprenorphine effects in experimental studies requiring prolonged opioid analgesia where rodent-specific formulations are unavailable, although further evaluation of safety, dosing, and generalizability is required.

PMID 42638138
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PubMedAnesthesia and pain medicine2026-08-25

An evaluation of transdermal buprenorphine and transdermal fentanyl patch on quality of recovery-15 and analgesic effect following inguinal hernia surgery: a randomized controlled study.

A Chaitanya Pratyusha CP, Ch Rama Krishna Prasad RKP, Garre Sandeep S, S Kalyani Sdl KS et al.

Effective postoperative analgesia is essential for optimizing recovery and patient satisfaction after inguinal hernia surgery. Therefore, we compared transdermal buprenorphine and fentanyl patches with conventional analgesia for pain control and quality of recovery-15 (QoR-15). In this prospective, randomized study 150 patients classified as American Society of Anesthesiologists (ASA) I-III scheduled for elective open inguinal hernia repair were randomized into three groups; (n=50 each) Group B (buprenorphine 10 µg/h patch), Group F (fentanyl 25 µg/h patch), and Group C (intravenous paracetamol and tramadol). Patches were applied 12 h preoperatively. The primary outcome was visual analog scale (VAS) pain score, assessed at 1, 6, 12, and 24 h. Secondary outcomes included QoR‑15 scores and rescue‑analgesic requirements. Statistical analysis was performed using the Kruskal-Wallis and Mann-Whitney U tests with Bonferroni correction. Baseline demographic characteristics and perioperative hemodynamic parameters were comparable across groups. Median postoperative VAS scores at 6, 12, and 24 h were significantly lower in both transdermal groups than in the control group. QoR-15 scores at 24 h were 124 (122-125) (C), 127 (125-129) (F), and 133 (131-134) (B), at 48 h were 129 (128-130), 136 (134-138), and 137 (135-139) for Groups C, F, and B, respectively (P = 0.001). Transdermal buprenorphine and fentanyl provided effective postoperative analgesia and were associated with improved quality of recovery compared with standard analgesia. Buprenorphine showed a significant advantage over fentanyl in QoR-15 at 24 h, however, this difference was not significant at 48 h.

PMID 42638571
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PubMedMedicinal research reviews2026-08-25

Developing the Dopamine D3 Receptor (D3R) Antagonist, (R)-VK4-116, as a Non-Opioid Medication for the Treatment of Opioid Use Disorder.

Wu Chia-Kuei CK, Lin Yu-Chih YC, Huang Junfeng J, Ding Bangwei B et al.

Opioid use disorder (OUD) remains a major global health challenge, and currently approved treatments (methadone, buprenorphine, and naltrexone) are all opioid receptor-targeting drugs with limitations in access, adherence, stigma, and use in polysubstance use disorders. Because the dopamine D3 receptor (D3R) is enriched in limbic brain regions involved in reward, drug dependence, and impulse control, it has become an attractive target for treating OUD and related substance use disorders. This review first surveys the emerging field of D3R antagonists as non-opioid therapeutics for substance use disorders, including D3R-selective compounds that have advanced into clinical development. We then present VK4-116 as a representative case study of translational progress in this field. Guided by D3R crystal structure-based modeling and medicinal chemistry optimization, VK4-116 was identified as a highly D3R-selective antagonist with favorable brain penetration and in vivo activity. In rodent models, VK4-116 reduced opioid self-administration, drug seeking, withdrawal-induced hyperalgesia, and irritability-like behavior, while enhancing opioid analgesia and reversing cocaine-induced cognitive deficits. The eutomer, (R)-VK4-116, was advanced through preclinical development, including scalable good manufacturing practices-compatible synthesis, formulation optimization to improve oral bioavailability, and investigational new drug-enabling toxicology studies defining toxicity endpoints, the no observed adverse effect level, and a safe clinical starting dose. Together, these findings support clinical evaluation of (R)-VK4-116 and illustrate the therapeutic promise of D3R antagonists for OUD and polysubstance use disorders.

PMID 42640111
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PubMedEuropean journal of nuclear medicine and molecular imaging2026-08-22

Total-body [11C]carfentanil PET: Liver-brain axis in methadone vs. buprenorphine treatment.

Li Elizabeth J EJ, Wiers Corinde E CE, Hsieh Chia-Ju CJ, Lee Hsiaoju H et al.

To examine the relationship between brain mu opioid receptor (MOR) availability and liver activity in opioid use disorder (OUD) patients treated with methadone (MET) or buprenorphine (BUP). 10 OUD patients, 5 treated with MET and 5 with BUP, as well as 13 healthy controls (HCs) underwent total-body PET [11C]carfentanil (CFN) imaging. MOR availability was quantified using distribution volume ratio (DVR) in key MOR-rich brain regions, and hepatic distribution volume (Vt) was used as an index of systemic tracer pharmacokinetics. Serum drug levels were measured in the OUD patients. Brain MOR availability was significantly lower in the OUD groups relative to HCs (p < 0.001), more so in BUP-treated (mean MOR difference = 39.9 ± 15.9%, Cohen's d = 3.35) than MET-treated (mean MOR difference = 14.2 ± 9.9%, d = 1.90) patients. Central MOR availability was inversely related to serum drug levels, linearly in MET treated (R2 = 0.83) and logarithmically in BUP-treated (R2 = 0.96), consistent with distinct receptor occupancy dynamics. Hepatic Vt differed across groups (p < 0.003) with levels in both OUD groups lower than in HCs (p < 0.05). In MET-treated patients, hepatic Vt was strongly associated with brain MOR availability (R2 = 0.68), and inversely associated with serum drug levels (R2 = 0.63). This relationship was less pronounced in BUP-treated patients (R2 = 0.30), and absent in HCs. Drug-specific, brain-liver pharmacokinetic profiles were observed in OUD patients treated with MET versus BUP. While MET patients demonstrated coupling between hepatic tracer kinetics and brain receptor occupancy, BUP patients did not. These findings demonstrate that drug-specific brain-body pharmacokinetics may underscore observed clinical differences in opioid agonist effects in OUD.

PMID 42631870
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PubMedmedRxiv : the preprint server for health sciences2026-08-20

What constitutes safe and effective dose titration of methadone and buprenorphine/naloxone? protocol for a population-based target trial emulation.

Mondol Momenul Haque MH, Zanette Michelle M, Min Jeong Eun JE, Kurz Megan M et al.

Clinical guidelines for managing opioid use disorder (OUD) recommend incremental dose titration for methadone and buprenorphine/naloxone to achieve a safe therapeutic maintenance dose. Dose titration recommendations are based on clinical experience, pharmacologic rationale, and expert consensus, with limited real-world evidence, especially in settings with widespread fentanyl use, where traditional titration schedules may be insufficient to address the higher opioid tolerance among people initiating treatment. This study aims to determine the comparative effectiveness of alternative titration schedules on completed induction and time to all-cause mortality. We will conduct a population-based retrospective cohort study using linked data from nine provincial health administrative databases. The study population will include adults (≥18 years) in British Columbia, Canada, who initiated methadone or buprenorphine/naloxone between 01/01/2010 and 30/06/2022. Primary outcomes are completed induction (defined as no dose increase for ≥two weeks without any intervening decrease) and time to all-cause mortality, with overdose-related acute care visits or overdose-related death and treatment discontinuation as secondary outcomes. Using a target trial framework, this study will implement a 'clone-censor-weight' approach to estimate the per-protocol effects of sustained titration schedules capturing adherence to and deviation from clinical guidelines. Sensitivity analyses will assess the robustness of findings through cohort and timeline restrictions as well as alternative exposure and outcome definitions. This study will generate real-world evidence on the comparative effectiveness of alternative titration schedules of methadone and buprenorphine/naloxone on completed induction and all-cause mortality. The findings will support evidence-informed updates to OAT guidelines and clinical decision-making in British Columbia and other jurisdictions facing escalating opioid-related harms.

PMID 42619818
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PubMedResearch square2026-08-20

How should low-threshold and primary care clinics prepare to provide long-acting injectable buprenorphine? A qualitative implementation study of patient and staff perspectives.

Jakubowski Andrea A, Lamont Isabel I, Huxley-Reicher Zina Z, Patel Viraj V VV et al.

Background Many patients with opioid use disorder (OUD) could benefit from long-acting injectable buprenorphine (LAIB), but it is not broadly available. This study examined the implementation of LAIB in three clinics (one primary care and two "low-threshold" clinics at syringe services programs (SSP)). Objectives were to identify implementation determinants (i.e., barriers and facilitators) at the organization, staff, and patient levels to inform development of tailored implementation strategies for each setting. Methods Researchers conducted semi-structured, qualitative interviews with staff (N = 23) and people with OUD who had lived experience with buprenorphine (N = 15) during early LAIB implementation at one primary care and two low-threshold clinics in New York City. Meeting notes from multidisciplinary clinical implementation working groups with staff (N = 27) served as an additional data source. Qualitative data collection and subsequent rapid qualitative analysis focused on implementation determinants by CFIR domain: the Innovation (LAIB), Individuals (staff and people with OUD), Inner Setting (organizational factors), and Outer Setting (external to where implementation is taking place), and recommendations for developing implementation strategies. Results In the Individuals domain, although staff were generally enthusiastic about implementing LAIB, they lacked comfort in counseling about LAIB, which necessitated tailored training and ongoing support. People with OUD expressed a need for detailed information about LAIB (e.g., side effects, withdrawal experiences, duration of effect) and suggested a peer messenger as an information source. Strong leadership support, clinical champions, and prior experience with sublingual buprenorphine helped overcome challenges in the Inner Setting. In the Outer Setting, the requirements to obtain LAIB from specialty pharmacies and federal regulations regarding controlled substance storage posed challenges for clinics. Conclusions In examining early implementation of LAIB in primary care and low-threshold clinics, multi-level barriers were identified as targets for implementation strategy development, including staff training needs, pharmacy access, and regulatory requirements. Favorable staff attitudes, strong leadership support, and local clinical champions helped overcome implementation barriers. These results can guide clinics in choosing implementation strategies and strengthen readiness for successful integration of LAIB.

PMID 42620108
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