Delving into the Latest Updates on Pelubiprofen with Synapse

Although drugs such as acetaminophen, opioids, and nonsteroidal anti-inflammatory drugs (NSAIDs), are commonly used for pain management, the side effects of these drugs such as hepatotoxicity, nephrotoxicity, nausea, and vomiting, can not be neglected. Therefore, combinations of analgesics with different mechanisms raise the possibility of developing novel analgesics. Therefore, the aim of the present study was to evaluate whether DW-1021, the ionic complex of pelubiprofen (NSAID) and tramadol (opioid), has synergic antinociceptive and anti-inflammatory effects in nociceptive as well as inflammation-induced nociceptive models compared to pelubiprofen- or tramadol-only administration. Strong synergistic antinociceptive efficacy of DW-1021 was observed in the mouse writhing test and von Frey paw withdrawal threshold test in the carrageenan-induced rats. The hot plate test in mice and the Randall-Selitto mechanical paw pressure test in carrageenan-induced rats revealed that DW-1021 had a preferable effect on relieving pain to pelubiprofen, but not as much as tramadol. In the carrageenan-induced rats, DW-1021 had a more potent effect on reducing paw inflammation (paw volume, width, and thickness) via the suppression of PGE₂ production than tramadol, but less than that of pelubiprofen. Taken together, our results suggest that the administration of DW-1021, a combination of pelubiprofen and tramadol, exerted a potent effect and can be used as a potential therapeutic agent for relieving pain and inflammation.

19 Apr 2023·Pharmaceutics

Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy Subjects

Article

Author: Park, Hyeon-Jeong ; Kim, Ha-Yeon ; Hwang, Jun-Gi ; Jang, Ye-Lim ; Kim, Yu-Kyong ; Seo, Ji-Hyung ; Choi, Young-Sim ; Son, Yu-Jeong ; Park, Min-Kyu

Compared to pelubiprofen, a cyclooxygenase-2-selective inhibitor, pelubiprofen tromethamine has been reported to exhibit improved solubility and absorption.Pelubiprofen tromethamine combines the anti-inflammatory effect of pelubiprofen with the gastric protective function of tromethamine salt, making it a relatively safe class of non-steroidal anti-inflammatory drugs with low levels of gastrointestinal side effects in addition to its original analgesic, anti-inflammatory, and antipyretic effects.This study assessed the pharmacokinetic and pharmacodynamic characteristics of pelubiprofen and pelubiprofen tromethamine in healthy subjects.Two independent clin. trials were performed in healthy subjects using a randomized, open-label, oral, single-dose, two-sequence, four-period, crossover design.In Study I and Study II, subjects received 25 mg of pelubiprofen tromethamine and 30 mg of pelubiprofen tromethamine, resp., with 30 mg of pelubiprofen being the referenceStudy I fell within the bioequivalence study criteria.A trend of increased absorption and exposure for 30 mg of pelubiprofen tromethamine vs. the reference in Study II was observedThe maximum cyclooxygenase-2 inhibitory effect of 25 mg of pelubiprofen tromethamine was approx. 98% compared to the reference, showing no significant pharmacodynamic variation.It is thus predicted that 25 mg of pelubiprofen tromethamine would show no clin. significant discrepancies in clin. analgesic and antipyretic effects from 30 mg of pelubiprofen.

01 Jan 2020·Yonsei Medical Journal

A Case of Vanishing Bile Duct Syndrome after Drug-Induced Liver Injury Caused by Pelubiprofen

Author: Lee, Young-Sun ; Lee, Yoonseok ; Kim, Hayeon ; Bak, Haein ; Bang, Soo-Min ; Lee, Sieun

Vanishing bile duct syndrome (VBDS) is a rare disease characterized by ductopenia and cholestasis, and is linked to immunological damage to the bile duct system. VBDS can be triggered by infection, ischemia, autoimmune diseases, adverse drug reactions, and humoral factors associated with malignancy. A few cases of VBDS associated with nonsteroidal anti-inflammatory drug-related drug-induced liver injury (DILI) have been reported. Here, we report a case of a 29-year-old patient who developed DILI that progressed to VBDS after the administration of pelubiprofen.

100 Deals associated with Pelubiprofen

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KEGG	Wiki	ATC	Drug Bank
D01865	-	M01AE	DB12150

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Back Pain	KR	Daewon Pharmaceutical Co., Ltd.	01 Dec 2008
Osteoarthritis	KR	Daewon Pharmaceutical Co., Ltd.	01 Dec 2008

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Rheumatic Diseases	Phase 2	US	Daiichi Sankyo Co., Ltd.	-
Rheumatic Diseases	Phase 2	JP	Daiichi Sankyo Co., Ltd.	-
Primary dysmenorrhea	Preclinical	-	Daewon Pharmaceutical Co., Ltd.	30 Sep 2020
Wounds and Injuries	Preclinical	KR	Daewon Pharmaceutical Co., Ltd.	25 Feb 2019
Back Pain	Preclinical	-	Daewon Pharmaceutical Co., Ltd.	01 Apr 2014
Acute upper respiratory infection	Preclinical	KR	Daewon Pharmaceutical Co., Ltd.	01 Jan 2013
Fever	Preclinical	KR	Daewon Pharmaceutical Co., Ltd.	01 Jan 2013
Musculoskeletal Pain	Preclinical	KR	Daewon Pharmaceutical Co., Ltd.	-
Rheumatoid Arthritis	Preclinical	KR	Daewon Pharmaceutical Co., Ltd.	-
Acute Pain	Discovery	KR	Daewon Pharmaceutical Co., Ltd.	-