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Quickly find freely available drug and population models in our PBPK model repository.

The models provided have been collated from published examples which authors have shared in our Published Model Collection or developed as part of various global health projects in our Global Health Collection. This search facility searches both model collections simultaneously.

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Found 126 Matches

Mefloquine

Model Files Publication

Brand Name(s) include: Lariam, Mephaquin, Mefliam

Disease: Malaria

Drug Class: Antimalarials

Date Updated: November 2021

The model at-a-glance

Absorption Model	First-Order
Volume of Distribution	Full PBPK (Method 2)
Route of Elimination	CYP3A4 (fm =100); renal clearance (fe = 0.05)
Perpetrator DDI	CYP2C9 Inhibitor CYP2D6 Inhibitor CYP3A4 Inhibitor
Validation	Six clinical studies describing single and multiple dose exposure of mefloquine were used the verify the PBPK model. Most of the studies (83%) were within 1.5-fold, with all simulations falling within 2-fold of the observed values. Two clinical DDI studies where mefloquine was the victim of a CYP3A4-mediated DDI were accurately recovered using the PBPK model.
Limitations	Only profiles of plasma concentrations assessed, many studies report blood concentrations Mefloquine has significant uptake into erythrocytes and haematocrit levels typically not reported Could be important in disease population (Possible time-varying B/P for Malaria patients?) Cmax for doses > 750 mg over predicted fa possibly decreases with dose, more data needed to fully determine the cause Most literature data extracted from graphs of mean data, difficulty determining accurate early time points due to poor image quality Verification needed for perpetrator DDI assessment as literature data is unavailable at this time
Updates in V19	Updated in vitrodata fu_p: 0.016 -> 0.015 B:P ratio 1.7 -> 1.1 and subsequent re-calculation of CLint using the retrograde approach Converted model to full PBPK distribution model with Vss predicted through Method 2 Sensitivity analysis of ka

Search Score: 1

Avibactam_V15R1_USFDA_20170810

Model Files Publication

http://onlinelibrary.wiley.com/doi/10.1002/cpt.750/full Avibactam compound file in healthy volunteers. Evaluation of the effect of renal impairment on PK of OAT substrates

Search Score: 1

Bergamottin_V19R1_AstraZeneca_20210423

Model Files Publication

CYP inhibitor found in grapefruit juice. AstraZeneca file.

Search Score: 1

Cefuroxime_V12R1_FDA_20150709

Model Files Publication

Table 1 of main paper and further discussion in supplemental file. IV only. Key feature is the use of mechanistic kidney model to simulate the effect of severe renal impairment and probenecid inhibition.

Search Score: 1

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Mefloquine

The model at-a-glance

Avibactam_V15R1_USFDA_20170810

Bergamottin_V19R1_AstraZeneca_20210423

Cefuroxime_V12R1_FDA_20150709

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