Drug intelligence / Profile preview

nalbuphine + ketorolac + dexamethasone + ondansetron

Development stage
Preclinical
Lead developer
Endo International
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

This is a combination drug consisting of four active pharmaceutical ingredients: - **Nalbuphine** is an opioid analgesic with mixed agonist-antagonist activity, primarily acting as a kappa-opioid receptor agonist and mu-opioid receptor antagonist. It provides moderate to severe pain relief. - **Ketorolac** is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis and providing potent analgesic and anti-inflammatory effects. - **Dexamethasone** is a synthetic glucocorticoid corticosteroid with strong anti-inflammatory and immunosuppressant properties. It also has notable efficacy in preventing nausea and vomiting when used perioperatively or during chemotherapy[1][2][3][5]. - **Ondansetron** is a selective serotonin 5-HT3 receptor antagonist used to prevent nausea and vomiting associated with surgery, chemotherapy, or radiation therapy[6][7][8][9]. The combination of these agents targets both pain control (nalbuphine, ketorolac) and prevention of postoperative or treatment-related nausea/vomiting (dexamethasone, ondansetron), making it suitable for perioperative care or settings where both analgesia and antiemetic prophylaxis are required[1][2][3][5].

02

Targets

KOR (Kappa opioid receptor)HTR3A (5-hydroxytryptamine receptor 3A)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)MOR (Mu opioid receptor)GR (Glucocorticoid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)

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