Drug intelligence / Profile preview

pacritinib + caffeine + midazolam + omeprazole + digoxin + rosuvastatin + metformin

Development stage
Phase 1
Lead developer
Sobi
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination drug consisting of **pacritinib**, **caffeine**, **midazolam**, **omeprazole**, **digoxin**, **rosuvastatin**, and **metformin**. - **Pacritinib** is a selective oral multikinase inhibitor primarily targeting JAK2 and FLT3, approved for the treatment of adults with intermediate or high-risk myelofibrosis with severe thrombocytopenia[2][1][6][7]. - **Caffeine** is a central nervous system stimulant that acts as an adenosine receptor antagonist. - **Midazolam** is a short-acting benzodiazepine used as a sedative and anxiolytic that acts as a GABA-A receptor positive allosteric modulator. - **Omeprazole** is a proton pump inhibitor that reduces gastric acid secretion by inhibiting the H+/K+ ATPase in stomach parietal cells. - **Digoxin** is a cardiac glycoside that inhibits Na+/K+ ATPase, increasing intracellular calcium and myocardial contractility. - **Rosuvastatin** is an HMG-CoA reductase inhibitor (statin) used to lower cholesterol. - **Metformin** is an antihyperglycemic agent that decreases hepatic glucose production and increases insulin sensitivity. Such combinations are mostly used for drug-drug interaction studies and not for clinical therapy. The main mechanism of each ingredient remains unchanged, and the combination allows assessment of metabolism and pharmacokinetics when taken together.

02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)IRAK1 (Interleukin-1 receptor-associated kinase 1)JAK2 (Janus kinase 2)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)ADOR (Adenosine receptors)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)ND1 (Mitochondrial electron transport chain complex I)ATP4A (Potassium–transporting ATPase alpha chain 1)ATP1A1 (Sodium/potassium-transporting ATPase subunit alpha-1)

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