Drug Discovery Process. BIT 120. ACE Inhibitors. Angiotensin Converting Enzyme (ACE) causes constriction of blood vessels by converting angiotensin from inactive to active form – want to block this enzyme, so blood vessels relax (Better blood flow, lower b.p.)
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Angiotensin Converting Enzyme (ACE)
causes constriction of blood vessels by converting angiotensin from inactive to active form – want to block this enzyme, so blood vessels relax (Better blood flow, lower b.p.)
Look for inhibitors to other ACE proteins
Class of drugs – end in “pril” – Captopril, etc.
Search Public Genome Databases for similar (homologous)
sequences to original ACE gene
Take these snippets and hybridize with genetic material from different tissues
Matches LIGHT up.
Clone the genes that light up
A. Laboratory and animal studies 6 yrs
B. File Investigational New Drug (IND)
C. Phases I- III 7 years
D. File New Drug Application (NDA)
at FDA: 1.5 years
E. Phase IV (post approval) 6 years
IND components – Goes into effect after 30 days if FDA says nothing
Toxicity in animals
$500 million/drug (dropping due to genomics)
5000 : 1
15 years chemical drug
10 years biological drug
how quickly drug is absorbed
eliminated from body (clearance)
Delivery Problem – injection vs. oral delivery
Do patients develop tolerance?
Interfere with meds for other diseases – eg. Lower bp
but interfere with med for type II diabetes
Good Laboratory Practices (GLP)
Good Manufacturing Practices (GMP)
Standard Operating Practices (SOP)
Documentation, Documentation, Documentation