Review
Pharmacology & Pharmacy
R. Yazbeck, S. E. Jaenisch, C. A. Abbott
Summary: DPP-4 inhibitors are small molecule inhibitors that prolong the insulinotropic activity of GLP-1 and are highly effective for treating Type-2 diabetes. Recent evidence suggests that DPP-4 inhibitors may also have immunomodulatory effects, particularly on aspects of innate immunity. Further research on the use of DPP-4 inhibitors in the context of the COVID-19 pandemic is highlighted.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Respiratory System
David Cipolla, Jimin Zhang, Brice Korkmaz, James D. Chalmers, Jessica Basso, Daniel Lasala, Carlos Fernandez, Ariel Teper, Kevin C. Mange, Walter R. Perkins, Eugene J. Sullivan
Summary: The research found that treatment with brensocatib can reduce the activity of NE, PR3, and CatG in sputum in patients with NCFBE, and it has a broad anti-inflammatory effect.
RESPIRATORY RESEARCH
(2023)
Article
Immunology
Yuichiro Iwamoto, Takatoshi Anno, Katsumasa Koyama, Fumiko Kawasaki, Kohei Kaku, Koichi Tomoda, Seiko Sugiyama, Yumi Aoyama, Hideaki Kaneto
Summary: DPP-4 inhibitors are closely associated with bullous pemphigoid (BP) and may lead to disruption of immune tolerance. Checking autoimmune antibodies may be important in DPP-4i-related BP, even when symptoms improve.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Pharmacology & Pharmacy
Jessica Basso, Kuan-Ju Chen, Yuchen Zhou, Lilly Mark, Daniel LaSala, Arielle Dorfman, Mary Atalla, Donald Chun, Veronica Viramontes, Christina Chang, Franziska Leifer, Patrick P. McDonald, David C. Cipolla
Summary: Brensocatib is a reversible inhibitor of DPP1 that inhibits the activation of NSPs, reducing damaging inflammation and potentially treating neutrophil-mediated inflammatory and autoimmune diseases.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Cell Biology
Yixin Tong, Yuan Huang, Yuchao Zhang, Xiangtai Zeng, Mei Yan, Zhongsheng Xia, Dongming Lai
Summary: DPP3 plays an oncogene-like role in the development and progression of CRC by targeting CDK1, which is correlated with lymphatic metastasis, pathological stage, and number of positive lymph nodes. Downregulation of DPP3 inhibits cell proliferation, migration and promotes apoptosis by upregulating multiple apoptosis-related genes.
CELL DEATH & DISEASE
(2021)
Article
Biochemistry & Molecular Biology
Shen-Chih Wang, Xiang-Yu Wang, Chung-Te Liu, Ruey-Hsing Chou, Zhen Bouman Chen, Po-Hsun Huang, Shing-Jong Lin
Summary: Linagliptin exhibits protective effects against endothelial inflammation and microvascular thrombosis in a mouse model of sepsis, and these effects are independent of blood glucose level.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
In Sun Goak, Jin A. Lee, Min Ho Jeong, Seol Ju Moon, Min Gul Kim
Summary: This study compared the pharmacokinetics of two fixed-dose combination (FDC) formulations in healthy Korean subjects. The results showed that the test FDC drug was equivalent to the reference FDC drug and both formulations were safe and well tolerated.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Article
Oncology
Yansen Xiao, Min Cong, Jiatao Li, Dasa He, Qiuyao Wu, Pu Tian, Yuan Wang, Shuaixi Yang, Chenxi Liang, Yajun Liang, Jili Wen, Yingjie Liu, Wenqian Luo, Xianzhe Lv, Yunfei He, Dong-Dong Cheng, Tianhao Zhou, Wenjing Zhao, Peiyuan Zhang, Xue Zhang, Yichuan Xiao, Youcun Qian, Hongxia Wang, Qiang Gao, Qing-Cheng Yang, Qifeng Yang, Guohong Hu
Summary: The study reveals that tumor-secreted protease CTSC promotes breast-to-lung metastasis by regulating recruitment of neutrophils and formation of neutrophil extracellular traps.
Article
Pharmacology & Pharmacy
Ganyu Wang, Weiqiang Jing, Yuxuan Bi, Yue Li, Liang Ma, Hui Yang, Yuankai Zhang
Summary: The study identified neutrophil elastase (NE) as a significant factor in osteoarthritis (OA), inducing chondrocyte apoptosis and facilitating OA development via the caspase signaling pathway. Inhibition of NE showed potential as a therapy for OA by mitigating chondrocyte apoptosis and pathological processes in vivo.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Biotechnology & Applied Microbiology
K. M. Khomtchouk, L. I. Joseph, B. B. Khomtchouk, A. Kouhi, S. Massa, A. Xia, I. Koliesnik, D. Pletzer, P. L. Bollyky, P. L. Santa Maria
Summary: This study identified Ly6G as the most informative factor driving disease in the CSOM mouse model, highlighting the role of neutrophils in the immune response. Neutrophil-specific immunomodulatory treatment significantly reduced bacterial burden in this model. Elevated levels of dsDNA in middle ear effusion samples may serve as a molecular biomarker of treatment response.
NPJ BIOFILMS AND MICROBIOMES
(2021)
Article
Biochemistry & Molecular Biology
Marija Drakul, Sergej Tomic, Marina Bekic, Dusan Mihajlovic, Milos Vasiljevic, Sara Rakocevic, Jelena Dokic, Nikola Popovic, Dejan Bokonjic, Miodrag Colic
Summary: Sitagliptin has an effect on the differentiation and maturation of human dendritic cells, with decreased expression of some immune activity molecules and increased expression of some tolerogenic molecules. Sitagliptin-treated cells have lower ability to stimulate T-cells and suppress certain T-cell responses while enhancing immunoregulatory responses. This effect may be achieved through the inhibition of NF-kB and p38MAPK expression.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Multidisciplinary Sciences
Tomoya Mita, Naoto Katakami, Hidenori Yoshii, Tomio Onuma, Hideaki Kaneto, Takeshi Osonoi, Toshihiko Shiraiwa, Tetsuyuki Yasuda, Yutaka Umayahara, Tsunehiko Yamamoto, Hiroki Yokoyama, Nobuichi Kuribayashi, Hideaki Jinnouchi, Masahiko Gosho, Iichiro Shimomura, Hirotaka Watada
Summary: This study investigated whether early initiation of alogliptin improved long-term cardiovascular outcomes. The results showed that early use of alogliptin was not associated with a reduced risk of composite cardiovascular disease, which could be attributed to fewer events and/or the addition of DPP-4 inhibitors during the follow-up period.
SCIENTIFIC REPORTS
(2023)
Article
Biochemistry & Molecular Biology
Dejan Agic, Maja Karnas, Sanja Tomic, Mario Komar, Zrinka Karacic, Vesna Rastija, Drago Beslo, Domagoj Subaric, Maja Molnar
Summary: This study investigated the inhibitory activity of 27 quinazolinone-Schiff's bases against human DPP III and identified five most potent inhibitors. These compounds were found to bind to the central enzyme cleft and interact with residues of the substrate binding subsites to exert inhibitory effects. Additionally, molecular dynamics simulations provided valuable insights into the mechanism of inhibitor binding and stabilization.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Endocrinology & Metabolism
Qi Pan, Mingxia Yuan, Lixin Guo
Summary: Our study aimed to evaluate the relationship between incretin-based medications and the risk of major adverse cardiovascular events. We found that there is a linear exposure-response relationship, suggesting that higher doses of GLP-1 RAs and increased exposure may lead to better cardiovascular benefits.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Medicine, General & Internal
Agnes Kinyo, Anita Hanyecz, Zsuzsanna Lengyel, Dalma Varszegi, Peter Olah, Csaba Gyomorei, Endre Kalman, Timea Berki, Rolland Gyulai
Summary: This study found an association between DPP4i and bullous pemphigoid in European patients, showing that DPP4i-induced BP differs significantly from classical BP with less skin symptoms, mild erythema, normal or slightly elevated peripheral eosinophil count, and lower titers of BP180 autoantibodies. This is the first case series of DPP4i-related BP with a non-inflammatory phenotype among European patients.
JOURNAL OF CLINICAL MEDICINE
(2021)
Article
Pharmacology & Pharmacy
Michael Gillen, Pablo Forte, Jan Olof Svensson, Rosa Lamarca, Joanna Burke, Karolina Rask, Ulrika Larsdotter Nilsson, Goran Eckerwall
PULMONARY PHARMACOLOGY & THERAPEUTICS
(2018)
Article
Allergy
Ubaldo J. Martin, Rainard Fuhr, Pablo Forte, Peter Barker, Milton J. Axley, Magnus Aurivillius, Li Yan, Lorin Roskos
Summary: The pharmacokinetic exposure of benralizumab following subcutaneous administration with either autoinjectors (AI) or accessorized prefilled syringes (APFS) was comparable. There were minor differences in exposure when comparing injection sites or weight classes, but clinically relevant outcomes, such as consistent blood eosinophil count depletion, were achieved with both devices. This suggests that patients and physicians have the flexibility to choose between AI and APFS for at-home delivery of benralizumab.
Article
Medicine, Research & Experimental
Andrew Whittaker, Asa M. Kragh, Judith Hartleib-Geschwindner, Muna Albayaty, Anna Backlund, Peter J. Greasley, Maria Heijer, Magnus Kjaer, Pablo Forte, Robert Unwin, Linda Wernevik, Hans Ericsson
CTS-CLINICAL AND TRANSLATIONAL SCIENCE
(2020)
Article
Pharmacology & Pharmacy
Hans Ericsson, Karin Nelander, Maria Heijer, Magnus Kjaer, Eva-Lotte Lindstedt, Muna Albayaty, Pablo Forte, Maria Lagerstrom-Fermer, Stanko Skrtic
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT
(2020)
Article
Pharmacology & Pharmacy
Carol M. MacLean, Zona Godsafe, Pablo Soto-Forte, Finn Larsen
Summary: Teverelix trifluoroacetate is a decapeptide that competitively and reversibly binds to gonadotropin-releasing hormone receptors, resulting in rapid suppression of luteinizing hormone and follicle-stimulating hormone levels. The release characteristics of teverelix differ significantly between subcutaneous and intramuscular routes, with the latter showing more prolonged reductions in pharmacodynamic endpoints. Dosage, administration route, and injection site all impact the release of teverelix in the body.
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT
(2022)
Article
Pharmacology & Pharmacy
Marloes van Hout, Pablo Forte, Thomas B. Jensen, Cristina Boschini, Tine A. Baekdal
Summary: This study aimed to compare different dosing schedules for oral semaglutide and their effects on the concentration of the drug in the body. The results showed that shorter fasting times significantly reduced the exposure of semaglutide in the body compared to the recommended overnight fasting period. Therefore, this study further supports the current prescribing information that patients should take oral semaglutide after an overnight fast.
CLINICAL PHARMACOKINETICS
(2023)
Correction
Pharmacology & Pharmacy
Marloes van Hout, Pablo Forte, Thomas B. Jensen, Cristina Boschini, Tine A. Baekdal
CLINICAL PHARMACOKINETICS
(2023)