modelMasitinib
Extends from Pharmacolibrary.Drugs.ATC.L.L01EX06.
Information
| name: | Masitinib | |
| ATC code: | L01EX06 | route: | oral |
| compartments: | 1 | |
| dosage: | 12.5 | mg |
| volume of distribution: | 368 | L |
| clearance: | 10.2 | L/h |
| other parameters in model implementation | ||
Masitinib is a selective tyrosine kinase inhibitor targeting c-Kit, PDGFR, and other kinases. It is used mainly in clinical trials for oncology and inflammatory diseases and is approved for use in veterinary medicine for treating mast cell tumors in dogs. Masitinib is not currently approved for human use in the United States or European Union but has been under investigation for various cancers and disorders.
Pharmacokinetics
Pharmacokinetic parameters reported in healthy adult human volunteers after single oral administration.
References
Soria, JC, et al., & Armand, JP (2009). Phase 1 dose-escalation study of oral tyrosine kinase inhibitor masitinib in advanced and/or metastatic solid cancers. European journal of cancer (Oxford, England : 1990) 45(13) 2333–2341. DOI:10.1016/j.ejca.2009.05.010 PUBMED:https://pubmed.ncbi.nlm.nih.gov/19541476
Mitry, E, et al., & Raymond, E (2010). Safety and activity of masitinib in combination with gemcitabine in patients with advanced pancreatic cancer. Cancer chemotherapy and pharmacology 66(2) 395–403. DOI:10.1007/s00280-010-1299-8 PUBMED:https://pubmed.ncbi.nlm.nih.gov/20364428
Parameters
| Type | Name | Default | Description |
|---|---|---|---|
| Modelica.Units.SI.Mass | weight (from PK_1C) | 75 | patient weight (kg) |
| Modelica.Units.SI.SpecificVolume | VdPerKg (from PK_1C) | 0.9 | Volume of distribution (L/kg) |
| Modelica.Units.SI.MassFraction | F (from PK_1C) | 0.8 | bioavailiability (0-1) |
| Pharmacolibrary.Types.Clearance | Cl (from PK_1C) | 20 | clearance |
| Modelica.Units.SI.Time | adminTime (from PK_1C) | 60 | first administration time (s) |
| Modelica.Units.SI.Time | adminDuration (from PK_1C) | 600 | administration duration (s) |
| Modelica.Units.SI.Time | adminPeriod (from PK_1C) | 8*60*60 | period of administration (default 8 hours)(s) |
| Pharmacolibrary.Types.Mass | adminMass (from PK_1C) | 1000 | administration mass (mg) |
| Integer | adminCount (from PK_1C) | 8 | number of dose administered (1) |
| Pharmacolibrary.Types.Volume | Vd (from PK_1C) | VdPerKg*weight | Volume of distribution (m3) |
| Pharmacolibrary.Types.MassConcentration | Cmin (from PK_1C) | 0.004 | minimal therapeutic range |
| Pharmacolibrary.Types.MassConcentration | Cmax (from PK_1C) | 0.008 | minimal therapeutic range |
| Pharmacolibrary.Types.MassConcentration | Ctox_peak (from PK_1C) | 0.012 | toxicity peak level |
| Pharmacolibrary.Types.MassConcentration | Ctox_trough (from PK_1C) | 0.006 | toxicity trough level |
| Pharmacolibrary.Types.TransferRate | ka (from PK_1C_enteral) | 0.016666666666666666 | first order absorption rate |
| Modelica.Units.SI.Time | Tlag (from PK_1C_enteral) | 600 | delay between oral administration and absorption (default 10min) |
Connectors
| Type | Name | Default | Description |
|---|---|---|---|
| Types.ConcentrationOutput | C_central (from PK_1C) | ||
| Interfaces.ConcentrationPort_b | centralCPort (from PK_1C) |
Components
| Type | Name | Default | Description |
|---|---|---|---|
| Pharmacokinetic.NoPerfusedTissueCompartment | central (from PK_1C) | ||
| Pharmacokinetic.ClearanceDrivenElimination | elim (from PK_1C) | ||
| Sources.PeriodicDose | periodicDose (from PK_1C) | ||
| Modelica.Units.SI.Time | t1_2 (from PK_1C) | elimination half-life |
Revisions
- 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)