modelOlmutinib
Extends from Pharmacolibrary.Drugs.ATC.L.L01EB06.
Information
| name: | Olmutinib | |
| ATC code: | L01EB06 | route: | oral |
| compartments: | 1 | |
| dosage: | 300 | mg |
| volume of distribution: | 164 | L |
| clearance: | 201 | L/h |
| other parameters in model implementation | ||
Olmutinib is a third-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed for the treatment of patients with non-small cell lung cancer (NSCLC) harboring T790M EGFR mutations. It targets both activating and T790M resistance mutations. Olmutinib was granted conditional approval in South Korea, but its approval was later withdrawn due to safety concerns and limited efficacy.
Pharmacokinetics
Pharmacokinetic parameters were estimated for adult patients with advanced solid tumors and NSCLC following a single oral dose. No comprehensive published PK population model or parameters with all fields available. Estimates are based on available phase I PK summary data.
References
Noh, YS, et al., & Jang, IJ (2019). A safety, pharmacokinetic, pharmacogenomic and population pharmacokinetic analysis of the third-generation EGFR TKI, olmutinib (HM61713), after single oral administration in healthy volunteers. Basic & clinical pharmacology & toxicology 125(4) 370–381. DOI:10.1111/bcpt.13262 PUBMED:https://pubmed.ncbi.nlm.nih.gov/31125491
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)