Metaboliti u procjeni sigurnosti molekule kandidata za lijek

master's thesis

• Title (english): Metabolites in safety assessment of drug candidates
• Author: Vida Špoljar
• Mentor: Monika Barbarić (mentor)
• Committee member: Ivana Perković (predsjednik povjerenstva)
• Committee member: Monika Barbarić (član povjerenstva)
• Committee member: Miranda Sertić (član povjerenstva)
• Granter: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of medicinal chemistry); Zagreb
• Defense date and country: 2021-07-15, Croatia
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract

Razvoj lijeka obuhvaća niz ispitivanja molekula kandidata od kojih će eventualno jedna, ukoliko se zadovolje zahtjevi djelotvornosti i sigurnosti, proći registraciju i nakon niza godina primjenjivati se u praksi među pacijentima. Metabolizam kandidata za lijek može utjecati na njegov farmakološki ili toksični učinak, stoga se provodi niz ispitivanja kako bi se potvrdila sigurnost metabolita. FDA-MIST smjernice definiraju proceduru ispitivanja nastalih metabolita te nalažu da se ispituje sigurnost glavnih metabolita prisutnih u jednakoj ili većoj količini od 10% spojeva prisutnih u organizmu povezanih s molekulom kandidatom. Međutim, u praksi postoji niz izuzetaka u kojima metaboliti u količini i manjoj od 10% mogu biti potencijalno toksični. Svojstva metabolita u procjeni sigurnosti molekule kandidata za lijek ispituje se različitim metodama in vitro, in silico i in vivo, a njihov razvoj ovisi o napretku različitih tehnika.

Abstract (english)

The development of the drug encompasses a series of testing the candidate molecules, out of which perhaps one will, if the conditions of efficiency and safety are satisfied, pass the registration after many years, and be used in practice on patients. Metabolism of drug candidates can greatly influence pharmacological or toxic effect which is why a series of testing is done to confirm their safety. FDA-MIST guidelines determine the testing procedure of the formed metabolites and demand safety testing of the main metabolites present in an equal or larger quantity than 10% of the compounds present in the organism associated with the candidate molecule. However, in practice, there are numerous exceptions in which metabolites whose quantity amounts to less than 10% can be potentially toxic. The properties of metabolites in safety assessment of drug candidate molecules are examined by various methods in vitro, in silico and in vivo and their development depends on the progress of various techniques.

• Keywords: razvoj lijeka; metaboliti; molekula kandidat
• Keywords (english): drug development; metabolites; drug candidate
• Language: croatian
• URN:NBN: urn:nbn:hr:163:293633
• Study programme: Title: Pharmacy; Study programme type: university; Study level: integrated undergraduate and graduate; Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access
• Created on: 2022-02-08 14:19:06