The use of buprenorphine (methadone) for detoxification or induced bridging of opioid addicts with the introduction of thiophene hydrochloride tablets for relapse prevention treatment, as well as the observation of patients' tolerance to thiophene hydrochloride tablets under the established medication regimen, provide a basis for the design of dosing regimens for this target subject population in the Phase IIa trial.

Start Date-

Sponsor / Collaborator

Institute of Poisons and Drugs, Academy of Military Medical Sciences, PLA

[+1]

CTR20150565 / Not yet recruitingPhase 2

盐酸噻吩诺啡片预防阿片类依赖者脱毒后复吸有效性与安全性的多中心、双盲、随机对照II期临床研究

[Translation] A multicenter, double-blind, randomized controlled phase II clinical study on the efficacy and safety of thiophene hydrochloride tablets in preventing relapse in opioid addicts after detoxification

通过评价盐酸噻吩诺啡片在阿片类依赖者脱毒后预防复吸的有效性与安全性，为后续试验给药方案确定提供科学依据.

[Translation]

The effectiveness and safety of thiophene hydrochloride tablets in preventing relapse in opioid addicts after detoxification were evaluated to provide a scientific basis for determining the dosing regimen in subsequent trials.

Start Date-

Sponsor / Collaborator

Institute of Poisons and Drugs, Academy of Military Medical Sciences, PLA

[+1]

CTR20170446 / Not yet recruitingPhase 2

应用盐酸丁丙诺啡片诱导引入盐酸噻吩诺啡片用于阿片类依赖防复吸探索性研究方案

[Translation] An exploratory study on the use of buprenorphine hydrochloride tablets to induce the introduction of thienorphine hydrochloride tablets for the prevention of relapse in opioid dependence

确定通过丁丙诺啡舌下片脱毒/诱导，再引入盐酸噻吩诺啡片的临床桥接方案，为噻吩诺啡控制阿片类依赖复吸的临床研究做准备。

[Translation]

To determine a clinical bridging regimen of detoxification/induction with buprenorphine sublingual tablets followed by the introduction of thienorphine hydrochloride tablets, in preparation for clinical studies on thienorphine for controlling relapse of opioid dependence.

Start Date-

Sponsor / Collaborator

Institute of Poisons and Drugs, Academy of Military Medical Sciences, PLA

[+1]

100 Clinical Results associated with Thienorphine Hydrochloride

100 Translational Medicine associated with Thienorphine Hydrochloride

100 Patents (Medical) associated with Thienorphine Hydrochloride

Literatures (Medical) associated with Thienorphine Hydrochloride

01 Dec 2020·Brain ResearchQ4 · MEDICINE

Thienorphine induces antinociception without dependence through activation of κ- and δ-, and partial activation of μ- opioid receptor

Q4 · MEDICINE

Article

Author: Zhou, Peilan ; Su, Ruibin ; Chen, Ming ; Gong, Zehui ; Li, Yulei ; Zhang, Yixin ; Yong, Zheng

Thienorphine hydrochloride is a new anti-relapse drug for opioid abusers that is currently in phase II clinical trial. In the present study, the antinociception, dependence, and signal transduction induced by thienorphine were examined. Thienorphine showed a potent antinociception effect in acetic acid-induced writhing test and formalin test. In the hot plate test and tail-flick test, thienorphine presented the typical partial opioid agonist character with a ceiling dose-response curve in addition to a bell-shaped curve. The hot plate test revealed that thienorphine induced approximately 50% of antinociception in μ receptor knockout (μ-KO) mice compared to wild-type controls (P < 0.05). The κ, δ selective antagonist nor-binaltorphimine (nor-BNI), and naltrindole decreased approximately 50-60% of theinorphine antinociception in μ-KO mice, respectively. The ORL1 receptor-selective antagonist J113397 did not affect theinorphine antinociception in μ-KO mice. Chronic treatment with thienorphine (1.5 mg/kg) induced some tolerance that was lower compared to buprenorphine or morphine addition. In contrast to buprenorphine or morphine, thienorphine did not lead to psychological dependence by conditioned place preference (CPP). The maximum inhibition of thienorphine on protein kinase A (PKA) activity was about 36%, 100%, 100%, and 12% in CHO-μ/κ/δ/ORL1-PKAcatEGFP cells, respectively. Similar results were observed in cyclic adenosine monophosphate (cAMP) accumulation inhibited by thienorphine in cells. Thienorphine significantly increased pERK1/2 in CHO-κ/δ-PKAcatEGFP cells. These results indicated that thienorphine induced analgesia through activation of κ- and δ-, partial activation of μ- opioid receptor without a bias between G-protein- and β-arrestin-mediated pathways. Thienorphine might be used for antinociception with minimal adverse effects.

01 Oct 2016·European Journal of PharmacologyQ3 · MEDICINE

Effects of thienorphine on the contraction of isolated ureter and bladder of guinea pigs

Q3 · MEDICINE

Article

Author: Zhou, Peilan ; Li, Yulei ; Gong, Zehui ; Yan, Hui ; Su, Ruibin ; Yong, Zheng

Opioid analgesics are widely used in moderate to severe pain including renal colic. Morphine is believed to cause spasm of ureter and affect the bladder contractions. Thienorphine is a partial opioid agonist that is a good candidate for the treatment of opioid dependence and pain. This study examined the effects of thienorphine on the guinea pig isolated ureter and bladder. The contractile amplitude of isolated ureter induced by KCl (40mM) was not influenced by thienorphine or buprenorphine, whereas morphine increased the amplitude of the isolated ureter. Thienorphine, buprenorphine or naloxone concentration-dependently antagonized the isolated ureter contraction induced by morphine. Thienorphine (1.0-32.0μM) or buprenorphine (1.0-32.0μM) had no effects on the spontaneous or acetylcholine (Ach) induced contractions of isolated bladder, but decreased the amplitude of the contractions of isolated bladder at 100μM concentration. Morphine (0.1-3.2mM) concentration dependently increased the spontaneous movement and Ach (1μM) induced contractions of isolated bladder. The mRNA levels of μ receptor in the ureter and bladder was as the same as that in the frontal cortex. In comparison, the mRNA levels of κ receptor, δ receptor and N/OFQ receptor was fewer than that in the frontal cortex. In summary, thienorphine has little influence on the guinea pig isolated ureter and bladder compared with morphine, which may result in a lack of adverse renal colic effects.

23 Mar 2016·Drug DeliveryQ2 · MEDICINE

Preparation and in vitro evaluation of thienorphine-loaded PLGA nanoparticles

Q2 · MEDICINE

ArticleOA

Author: Mei, Xing Guo ; Yang, Yang ; Xie, Xiang Yang

Poly (d,l-lactic-co-glycolide) nanoparticles (PLGA-NPs) have attracted considerable interest as new delivery vehicles for small molecules, with the potential to overcome issue such as poor drug solubility and cell permeability. However, their negative surface charge decreases bioavailability under oral administration. Recently, cationically modified PLGA-NPs has been introduced as novel carriers for oral delivery. In this study, our aim was to introduce and evaluate the physiochemical characteristics and bioadhesion of positively charged chitosan-coated PLGA-NPs (CS-PLGA-NPs), using thienorphine as a model drug. These results indicated that both CS-PLGA-NPs and PLGA-NPs had a narrow size distribution, averaging less than 130 nm. CS-PLGA-NPs was positively charged (+42.1 ± 0.4 mV), exhibiting the cationic nature of chitosan, whereas PLGA-NPs showed a negative surface charge (-2.01 ± 0.3 mV). CS-PLGA-NPs exhibited stronger bioadhesive potency than PLGA-NPs. Furthermore, the transport of thienorphine-CS-PLGA-NPs by Caco-2 cells was higher than thienorphine-PLGA-NPs or thienorphine solution. CS-PLGA-NPs were also found to significantly enhance cellular uptake compared with PLGA-NPs on Caco-2 cells. An evaluation of cytotoxicity showed no increase in toxicity in either kind of nanoparticles during the formulation process. The study proves that CS-PLGA-NPs can be used as a vector in oral drug delivery systems for thienorphine due to its positive surface charge and bioadhesive properties.

100 Deals associated with Thienorphine Hydrochloride

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Opium Dependence	Phase 2	CN	Beijing Zidu Hongye Technology Development Co Ltd	18 Sep 2015
Opium Dependence	Phase 2	CN	Institute of Poisons and Drugs, Academy of Military Medical Sciences, PLA	18 Sep 2015
Opioid-Related Disorders	Phase 2	CN	Academy of Military Medical Sciences	-
Opium Dependence	Discovery	CN	Academy of Military Medical Sciences	18 Sep 2015

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