Piprant

The piprants are a class of substances within pharmacology that act as prostaglandin antagonists.

Piprant

The piprants are a class of substances within pharmacology that act as prostaglandin antagonists.

Properties

Schematic, simplified representation of the synthesis pathway and receptors (blue) of prostanoids (yellow); sites of action of piprants and other antagonists

The suffix -piprant was published in 2013 by the World Health Organization (WHO) for the International Non-proprietary Name of chemical compounds that target prostaglandin receptors (prostanoid receptors, PG receptors) and do not possess a prostanoid structure (i.e., a structure derived from prostanoic acid).[1] They do not interfere with prostaglandin synthesis, distinguishing them from COX inhibitors, which suppress the biosynthesis of prostanoids from arachidonic acid by inhibiting cyclooxygenases. COX inhibitors are used as analgesics and non-steroidal anti-inflammatory drugs.

The prostaglandin receptors are G-protein-coupled receptors acting as membrane receptors and are divided into the following five types with a total of nine subtypes: prostaglandin D2 receptor, prostaglandin E receptors, FP, IP, and the thromboxane receptor (TXA2R).[2]

The non-proprietary names of thromboxane receptor antagonists (TP antagonists) end in -troban.[1]

Representatives

Within the piprant class, the veterinary drug grapiprant, an EP4 receptor antagonist indicated in dogs for pain and inflammation associated with osteoarthritis, is approved for marketing.[3] The DP1 receptor antagonist laropiprant was used in human medicine until 2013 to suppress flush syndrome caused by treatment with the lipid-lowering drug nicotinic acid.[4]

Antagonists of the DP receptor include active substances against asthma,[2] as the DP2 subtype in particular (also known as CRTh2, an abbreviation for chemoattractant receptor homologous molecule on Th2 cells) mediates allergic reactions and is involved in inflammatory processes in allergic asthma.[5] Among the exclusively experimental representatives evaluated thus far, the development of the DP2 antagonists Fevipiprant, Vidupiprant, and Setipiprant as asthma medications failed,[6][7] while the development of Timapiprant showed mixed results.[7]

Chemical structure of Vorbipiprant

The therapeutic potential of EP4 antagonists is diverse and includes the treatment of inflammatory diseases, increased pain sensitivity (hyperalgesia), glaucoma, nephritis, and osteoporosis,[7] as well as diseases in the field of oncology.[8] Palupiprant and Vorbipiprant are under development for cancer immunotherapy.[9][10]

[Ebopiprant]] is an FP receptor antagonist (PGF2α receptor antagonist) being developed to delay preterm birth in pregnant women.[11]

References

  1. ^ a b "Pre-stems: Suffixes used in the selection of INN - October 2013". Retrieved 2026-05-08.
  2. ^ a b Takako Hirata, Shuh Narumiya (2011-10-12), "Prostanoid Receptors", Chemical Reviews, vol. 111, no. 10, pp. 6209–6230, doi:10.1021/cr200010h, PMID 21819041
  3. ^ Stephan Neudeck (February 2019), "Osteoarthritis beim Hund – Grapiprant als neue Therapieoption: Piprante wie Grapiprant (Galliprant®) bieten durch ihren selektiven Wirkansatz neue Potenziale für Hunde mit chronischen Gelenkerkrankungen", Kleintier Konkret, vol. 22, no. 1, pp. 47–50, doi:10.1055/a-0815-7389
  4. ^ "Das Aus für Nikotinsäure/Laropiprant zur Behandlung der Hyperlipidämie". Der Arzneimittelbrief (in German). 2013-03-01. Retrieved 2026-05-10.
  5. ^ Gerd Geisslinger, Thomas Gudermann, Burkhard Hinz, Aimo Kannt, Peter Ruth, Ursula Storch: Mutschler Arzneimittelwirkungen. Pharmakologie – Klinische Pharmakologie – Toxikologie. Begründet von Ernst Mutschler, 12. Auflage. Wissenschaftliche Verlagsgesellschaft, Stuttgart 2025, ISBN 978-3-8047-4506-3, S. 97.
  6. ^ GlobalData Healthcare (2019-12-23). "Novartis discontinues asthma drug candidate fevipiprant following another Phase III trial failure". Clinical Trials Arena. Retrieved 2026-05-08.
  7. ^ a b c Linda Zhu, Christina E. Ciaccio, Thomas B. Casale (2018), "Potential new targets for drug development in severe asthma", World Allergy Organization Journal, vol. 11, no. 1, doi:10.1186/s40413-018-0208-1, PMC 6203275, PMID 30386455{{citation}}: CS1 maint: multiple names: authors list (link)
  8. ^ Debasis Das, Dandan Qiao, Zhonghe Liu, Lingzhi Xie, Yong Li, Jingbing Wang, Jianhe Jia, Yuxi Cao, Jian Hong (2023-06-08), "Discovery of Novel, Selective Prostaglandin EP4 Receptor Antagonists with Efficacy in Cancer Models", ACS Medicinal Chemistry Letters, vol. 14, no. 6, pp. 727–736, doi:10.1021/acsmedchemlett.2c00495, PMC 10258902, PMID 37312837{{citation}}: CS1 maint: multiple names: authors list (link)
  9. ^ Diana I. Albu, Zichun Wang, Jiayi Wu, Kuan-chun Huang, Wei Li, Diana Liu, Galina Kuznetsov, Qian Chen, Xingfeng Bao, Mary Woodall-Jappe (2015-08-01), "Abstract 275: ER-886046, an antagonist of PGE2 receptor type-4, induces an effective antitumor immune response in mice by attenuating intratumoral MDSCs and TAMs", Cancer Research, vol. 75, no. 15_Supplement, p. 275, doi:10.1158/1538-7445.AM2015-275{{citation}}: CS1 maint: multiple names: authors list (link)
  10. ^ Filippo Pietrantonio, Federica Morano, Monica Niger, Filippo Ghelardi, Claudia Chiodoni, Michele Palazzo, Federico Nichetti, Paolo Manca, Eleonora Cristarella, Valentina Doldi, Nadia Zaffaroni, Giovanna Sabella, Nadia Brambilla, Elena Benincasa, Giampaolo Giacovelli, Cristina Vitalini, Federica Girolami, Lucio C. Rovati (2025-02-17), "The Prostaglandin EP4 Antagonist Vorbipiprant Combined with PD-1 Blockade for Refractory Microsatellite-Stable Metastatic Colorectal Cancer: A Phase Ib/IIa Trial", Clinical Cancer Research, vol. 31, no. 4, pp. 649–658, doi:10.1158/1078-0432.CCR-24-2611, PMC 11831105, PMID 39620921{{citation}}: CS1 maint: multiple names: authors list (link)
  11. ^ B.W. Mol, I. Fatkullin, L. Islamova, A. Parizek, H. Herman, P. Janku, T. Ho, T. Biron-Shental, A. Humberstone, E. Bestel, M. Brethous (2025), "Efficacy and safety of ebopiprant to delay preterm birth after oral administration in pregnant women with spontaneous preterm labor receiving atosiban: a phase 2a, double-blind, parallel group, randomized, placebo-controlled, proof of concept study", European Journal of Obstetrics & Gynecology and Reproductive Biology, vol. 313, doi:10.1016/j.ejogrb.2025.114637, PMID 40782442{{citation}}: CS1 maint: multiple names: authors list (link)

Content Disclaimer

Informasi ini disarikan dari Wikipedia dan disajikan kembali untuk tujuan edukasi. Konten tersedia di bawah lisensi CC BY-SA 3.0. Kami tidak bertanggung jawab atas ketidakakuratan data yang bersumber dari kontribusi publik tersebut.

  1. The information displayed on this website is sourced in part or in whole from Wikipedia and has been adapted for the purpose of restating it. We strive to provide accurate and relevant information, however:
  2. There is no guarantee of absolute accuracy. Wikipedia is an open, collaborative project that can be edited by anyone, so information is subject to change.
  3. It is not intended to constitute professional advice. The content displayed is for informational and educational purposes only. For important decisions (e.g., medical, legal, or financial), please consult a professional.
  4. Content copyright. Wikipedia is licensed under the Creative Commons Attribution-ShareAlike License (CC BY-SA). This means that content may be reused with appropriate attribution and shared under a similar license.
  5. Responsible use. Any risk arising from the use of information from this website is entirely the responsibility of the user.