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Small Molecule DMPK
ADME Services
- Physicochemical property
- Metabolic stability
- Distribution
- Permeability and transporter
- Drug-drug interaction (DDI)
- Customized assays
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High Quality of Physicochemical Property Evaluation
Kinetic SolubilityIn PBS, SGF, SIF
Thermodynamic SolubilityIn PBS, SGF, SIF
Chemical
StabilityIn PBS, SGF, SIF
Log D at pH7.4In octanol /buffer
Early Formulation ScreeningIn specific recipes -
Metabolic Stability with Variety of Capabilities
MicrosomalHumanICR mouse, SD ratBeagle dogCynomolgus monkeyHepatocyteHumanICR mouse, SD ratBeagle dogCynomolgus monkeyPlasmaHumanICR mouse, SD ratBeagle dogCynomolgus monkeyWhole bloodICR mouseSD ratStability challenges following oral administration -
Distribution Services with Reliable Results
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Reliable Permeability and Transporter Assays
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ADME Services for Drug-Drug Interaction(DDI)
CYP Inhibitor Substrate Reaction Metabolite 1A2 α-Naphthoflavon Phenacetin Phenacetin O-deethylation Acetaminophen 2B6 Clopidogrel Bupropion Bupropion-hydroxylation Hydroxybupropion 2C8 Nicardipine Paclitaxel Paclitaxel 6α-hydroxylation 6α-hydroxy Paclitaxel 2C9 Sulfaphenazole Diclofenac Diclofenac 4'-hydroxylation 4'-hydroxy diclofenac 2C19 Omerazole S-Mephenytoin s-Mephenytoin 4'-hydroxylation 4-Hydroxy Mephenytoin 2D6 Quinidine Dextromethorphan Dextromethorphan O-demethylation Dextrorphan 3A4-T Ketoconazole Testosterone Testosterone 6β-hydroxylation 6β-hydroxy Testosterone 3A4-M Ketoconazole Midazolam Midazolam 1-hydroxylation Mida1'-hydroxy Midazolam -
PK ServicesRat PKMouse BBB penetrationMouse PK: serial samplingCassette dosing PKMouse PK: parallel samplingDog PKRat BBB penetrationMTD study
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PK Services
AnimalRodent, non-rodentAdministrationIV/SC/IM/IP/POSamplesPlasma, blood, CSF, bile, other fluidsTissue distributionBrain, CSF for BBB penetration; liver,kidney, lung etc.ExcretionFecal, urine, bileDDIABT (CYP inhibitor)pH dependentPentagastrin, FamotidineP-gp inhibitionVerapamilStudy Type Workflow (Days) Rat PK 5 Mouse PK:serial
sampling5 Mouse PK:parallel sampling 5 Rat BBB
penetration#3 Mouse BBB
penetration#3 Cassette dosing pk 5 *standard pk with iv (1mpk), po (10 mpk), n=3# two time points for BBB penetration -
CNS Distribution and PK ProfilingNon-compartmental AnalysisParameter(IV)Lambda_zt1/2TmaxCmaxC0AUC 0-tAUC 0-inf_obsMRT 0-inf_obsCl_obsVss_obsLambda_zTmaxC0AUC 0-inf_obsCl_obst1/2CmaxAUC 0-tMRT 0-inf_obsVss_obsParameter(PO)Lambda_zt1/2TmaxCmaxAUC 0-tAUC 0-inf_obsMRT 0-inf_obsVz_obsFLambda_zTmaxAUC 0-inf_obsVz_obst1/2CmaxAUC 0-tMRT 0-inf_obsF
CNS exposure PKAUC brainBrain to plasma ratioKp=AUC 0-t bRain/AUC 0-T plasmaKp,uu=(Cbrain/Cplasma)*(Fubrain/FuPlasma)Kp,uu1 Passive BBB diffusion<1 Efflux at BBB>1 Uptake at BBB -
Experienced in Discrete and Cassette PK Studies
Discrete Cassette Advantages Disadvantages Advantages Disadvantages w/o drug interactions Many animals used Reduction in animal usage Possible drug interactions w/o Iimitation on dose size Many biological samples to assay Reduction in analytical sample input Doses must be kept small Many reports Complex LC-MS/MS method development -
DMPK Research for Peptide
