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Summary

Samenvatting non-cilnical drug development

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Dit is een korte samenvatting over het deel non-cilnical drug development

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  • January 6, 2024
  • 2
  • 2023/2024
  • Summary
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Non-clinical DD (Annaert)
ADME testing (vroege ontwikkeling)
 Absorptie
o Caco 2 (cancer colon cellen)
 Vormen laag  Papp meten  voorspelling fa (geabsorbeerde fractie) 
voorspelling F (biologische beschikbaarheid)
 Oppervlakte, concentratie en snelheid gekend  Papp  flux
 Flux: Papp (afh van log P) * initiële concentratie (afh van oplosbaarheid)
 1 celtype
 Geen mucuslaag
 Brengen ook transporters (bv. Pgp) tot expressie  beter dan enkel log P  ook
polariteit van transport bekijken  F voorspellen
o Oplosbaarheid in biorelevante media
 Distributie
 Metabolisme
o Cl prediction (microsomes, hepatocytes)
 Microsomen (microsomal stability screening)
 Vd gekend, K uit experiment  niet-renale klaring
 Screening voor CYP/UGT metabolism
 Eliminatiesnelheid verandert continu  naarmate dat er minder is
begint het trager te gaan  verval is exponentieel
 Geen bijdrage cytosolische enzymen en andere cellulaire processen bv.
transporters
 Hepatocyten (suspensie of cultuur)
 Klaring obv AUC
 Veel interindividuele variabiliteit (humaan)  gepoold
 Beperkte functionaliteit/viabiliteit na cryopreservatie + duur
 Corrigeren voor dynamische wisselwerking tussen serum en
hepatocyten  biorelevantie ↑
 In vivo Cl prediction
 Obv in vitro experimenten (IVIVE)
 Normaliseren voor mg proteïne (microsomen) of voor #cellen
(hepatocyten)
 Rekening houden met hepatic blood flow, protein binding (well-stirred
model)
o Impact of (hepatic) transporters
 Veel transporters (bv. Pgp)
 Oil-spin methode om opname in hepatocyten (enkel cellen) te bepalen
 Activiteit is belangrijk om te meten, mRNA komt hier niet altijd mee overeen
 Ontogeny = ontwikkeling van activiteit van een transporter
 HIV protease inhibitors
o DDI (CYP inhibition, induction)

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