[Translation] A single-center, randomized, open-label, single-dose, two-sequence, two-period, double-crossover bioequivalence study of ubenimex capsules (30 mg) in Chinese healthy subjects under fasting and fed conditions

主要研究目的：按有关生物等效性试验的规定，选择Nippon Kayaku Co., Ltd.为持证商的乌苯美司胶囊（商品名：Bestatin，规格：30mg）为参比制剂，对西安万隆制药股份有限公司生产并提供的受试制剂乌苯美司胶囊（规格：30mg）进行空腹和餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评估两种制剂在空腹和餐后给药条件下的生物等效性。次要研究目的：观察健康志愿受试者口服受试制剂乌苯美司胶囊（规格：30mg）和参比制剂乌苯美司胶囊（商品名：Bestatin，规格：30mg）的安全性。

[Translation]

Main purpose of study: According to the relevant provisions of bioequivalence test, Nippon Kayaku Co., Ltd. is the licensee of Ubenimex Capsules (trade name: Bestatin, specification: 30mg) as the reference preparation, and the test preparation Ubenimex Capsules (specification: 30mg) produced and provided by Xi'an Wanlong Pharmaceutical Co., Ltd. are conducted on fasting and postprandial human bioequivalence tests to compare whether the absorption rate and degree of the drug in the test preparation are within the acceptable range with the reference preparation, and to evaluate the bioequivalence of the two preparations under fasting and postprandial administration conditions. Secondary purpose of study: To observe the safety of oral administration of the test preparation Ubenimex Capsules (specification: 30mg) and the reference preparation Ubenimex Capsules (trade name: Bestatin, specification: 30mg) by healthy volunteers.

Start Date11 Oct 2023

Sponsor / Collaborator

Xian Wanlong Pharmaceutical Co. Ltd.

CTR20232253 / CompletedNot Applicable

乌苯美司胶囊在中国健康志愿者空腹及餐后给药条件下生物等效性试验

[Translation] Bioequivalence study of ubenimex capsules in Chinese healthy volunteers under fasting and fed conditions

主要研究目的本研究以成都苑东生物制药股份有限公司研制的乌苯美司胶囊（10mg/粒）为受试制剂，原研厂家日本化药株式会社生产的乌苯美司胶囊（10mg/粒，商品名：Bestatin®）为参比制剂，评估受试制剂和参比制剂在空腹和餐后给药状态下的生物等效性，为该药注册申报及临床用药提供参考依据。次要研究目的评价中国健康志愿者空腹和餐后条件下受试制剂乌苯美司胶囊（10mg/粒）和参比制剂Bestatin®（10mg/粒）安全性。

[Translation]

Main research purpose This study uses Ubenimex Capsules (10 mg/capsule) developed by Chengdu Yuandong Biopharmaceutical Co., Ltd. as the test preparation, and Ubenimex Capsules (10 mg/capsule, trade name: Bestatin®) produced by the original manufacturer Nippon Kayaku Co., Ltd. as the reference preparation to evaluate the bioequivalence of the test preparation and the reference preparation under fasting and postprandial administration conditions, and provide a reference basis for the registration application and clinical use of the drug. Secondary research purpose Evaluate the safety of the test preparation Ubenimex Capsules (10 mg/capsule) and the reference preparation Bestatin® (10 mg/capsule) under fasting and postprandial conditions in healthy Chinese volunteers.

Start Date13 Aug 2023

Sponsor / Collaborator

Chengdu Easton Biopharmaceuticals Co., Ltd.

JPRN-jRCT2031210707 / RecruitingPhase 2

Phase II Trial of Ubenimex Combined with Pembrolizumab + nab-Paclitaxel + Carboplatin for Untreated Patients with Advanced Squamous Non-Small Cell Lung Cancer: (UBE-Q) - UBE-Q

Start Date04 Jan 2023

Sponsor / Collaborator-

100 Clinical Results associated with LTA4H x APB

100 Translational Medicine associated with LTA4H x APB

0 Patents (Medical) associated with LTA4H x APB

Literatures (Medical) associated with LTA4H x APB

01 Apr 2020·Journal of Assisted Reproduction and GeneticsQ3 · MEDICINE

Obesity significantly alters the human sperm proteome, with potential implications for fertility

Q3 · MEDICINE

Article

Author: Pini, T ; Katz-Jaffe, M ; Russ, J ; Hansen, K C ; Parks, J ; Schoolcraft, W B ; Dzieciatkowska, M

PURPOSEIn men, obesity may lead to poor semen parameters and reduced fertility. However, the causative links between obesity and male infertility are not totally clear, particularly on a molecular level. As such, we investigated how obesity modifies the human sperm proteome, to elucidate any important implications for fertility.METHODSSperm protein lysates from 5 men per treatment, classified as a healthy weight (body mass index (BMI) ≤ 25 kg/m²) or obese (BMI ≥ 30 kg/m²), were FASP digested, submitted to liquid chromatography tandem mass spectrometry, and compared by label-free quantification. Findings were confirmed for several proteins by qualitative immunofluorescence and a quantitative protein immunoassay.RESULTSA total of 2034 proteins were confidently identified, with 24 proteins being significantly (p < 0.05) less abundant (fold change < 0.05) in the spermatozoa of obese men and 3 being more abundant (fold change > 1.5) compared with healthy weight controls. Proteins with altered abundance were involved in a variety of biological processes, including oxidative stress (GSS, NDUFS2, JAGN1, USP14, ADH5), inflammation (SUGT1, LTA4H), translation (EIF3F, EIF4A2, CSNK1G1), DNA damage repair (UBEA4), and sperm function (NAPA, RNPEP, BANF2).CONCLUSIONThese results suggest that oxidative stress and inflammation are closely tied to reproductive dysfunction in obese men. These processes likely impact protein translation and folding during spermatogenesis, leading to poor sperm function and subfertility. The observation of these changes in obese men with no overt andrological diagnosis further suggests that traditional clinical semen assessments fail to detect important biochemical changes in spermatozoa which may compromise fertility.

01 May 2019·Biochemical and Biophysical Research CommunicationsQ3 · BIOLOGY

The effects of curcumin, mangiferin, resveratrol and other natural plant products on aminopeptidase B activity

Q3 · BIOLOGY

Article

Author: Lafont, René ; Mahbouli, Mouna ; Ghélis, Thanos ; Darmon, Cécile ; Piesse, Christophe ; Foulon, Thierry ; Désert, Alexandre ; Cadel, Sandrine

Aminopeptidase B (Ap-B) is a Zn²⁺-aminopeptidase of the M1 family which is implicated, in conjunction with the nardilysin endoprotease, in the generation of miniglucagon, a peptide involved in the maintenance of glucose homeostasis. Other in vivo physiological roles have been established for this vertebrate enzyme, such as the processing of Arg-extended forms of human insulin and cholecystokinin 9 and the degradation of viral epitopes in the cytoplasm. Among M1 family members, Ap-B is phylogenetically close to leukotriene A₄ hydrolase (LTA₄H), a bi-functional aminopeptidase also able to transform LTA₄ in LTB₄ (a lipid mediator of inflammation). As the activities of LTA₄H are reported to be inhibited by resveratrol, a polyphenolic molecule from red wine, the effect of this molecule was investigated on the Ap-B activity. Several other active phenolic compounds produced in plants were also tested. Among them, curcumin and mangiferin are the most effective inhibitors. Dixon analysis indicates that curcumin is a non-competitive inhibitor with a Ki value of 46 μmol.L^-1. Dixon and Lineweaver-Burk representations with mangiferin show a mixed non-competitive inhibition with Ki' and Ki values of 194 μmol.L^-1 and 105 μmol.L^-1, respectively. At 200 μmol.L^-1, no significant effect was observed with caffeic, chlorogenic, ferulic, salicylic and sinapic acids as well as with resveratrol. Analyses on the 3D-structure of LTA₄H with resveratrol (pdb: 3FTS) and the Ap-B 3D-model allow hypothesis to explain theses results.

01 Jan 2019·Journal of Biological ChemistryQ2 · BIOLOGY

Withdrawal: Identification of human aminopeptidase O, a novel metalloprotease with structural similarity to aminopeptidase B and leukotriene A4 hydrolase

Q2 · BIOLOGY

Article

Author: Quesada, Víctor ; López-Otín, Carlos ; Sánchez, Luis M. ; Fueyo, Antonio ; Suárez, María F. ; Ugalde, Alejandro P. ; Díaz-Perales, Araceli

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