Drug intelligence / Profile preview

palonosetron + dexamethasone + carboplatin + paclitaxel + olanzapine

Development stage
Unknown
Lead developer
Helsinn
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of five drugs—palonosetron, dexamethasone, carboplatin, paclitaxel, and olanzapine—used primarily in the context of cancer chemotherapy. Palonosetron is a selective 5-HT3 receptor antagonist that prevents nausea and vomiting by blocking serotonin receptors in the central nervous system and gastrointestinal tract. Dexamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressant properties; it also enhances antiemetic efficacy when combined with other agents. Carboplatin and paclitaxel are cytotoxic chemotherapeutic agents used to treat various cancers; carboplatin forms DNA crosslinks leading to apoptosis, while paclitaxel stabilizes microtubules inhibiting cell division. Olanzapine is an atypical antipsychotic that blocks multiple neurotransmitter receptors (dopaminergic D2, serotonergic 5-HT2A/2C/3, muscarinic cholinergic, histamine H1) and has demonstrated efficacy as an antiemetic for chemotherapy-induced nausea and vomiting (CINV), especially when added to standard regimens[1][2][3][5]. This multi-drug regimen targets both tumor cells (carboplatin/paclitaxel) and CINV prevention (palonosetron/dexamethasone/olanzapine).

02

Targets

DNADRD2 (Dopamine D2 Receptor)GR (Glucocorticoid receptor)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR3A (5-hydroxytryptamine receptor 3A)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)TUBB (Tubulin (alpha and beta subunits))

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