Week 0 + 1 Flashcards
Drug Development Part 1
In-vitro and In-Vivo testing:
Basic Research, early discovery, pre clinical
Meant to establish drug safety and efficacy
Drug Development Part 2
Human testing: Clinical Development
Phase 1: 10s of people
Phase 2: 100s of people
Phase 3: 1000s of people
Drug Development Part 3
Data Review=> FDA Review
Drug Development Part 4
Surveillance: Post-market monitoring
What protein allows SARS-CoV-1 to infect humans that some animals do not have?
ACE2R Receptor
What enzyme, if blocked, would inhibit viruses from infecting humans?
RNA dependent polymerase
What is Log P
Measure of lipophilicity of a molecule. Known as the octanol/water partition coefficient. Octanol is a representative of a lipophilic environment. Log P correlates to drug absorption and distribution in the body
To classify a drug as soluble in water. The log P must be?
Less than 0.5
Lipinski’s rule of Five
Provides a basis of whether a chemical compound is likely to become a drug.
- A molecular weight under 500
- Fewer than 10 H-bond acceptors
- Fewer than 5 H-bond donors
- A C log P value less than 5
Define a hydrogen bond donor (HBD)
A functional group that provides the hydrogen required for a hydrogen bond (When a hydrogen is bonded to another element)
Define a hydrogen bond acceptor (HBA)
Functional group that provides the electron-rich atom required to interact with a hydrogen in a hydrogen bond (A good hba has to be electronegative and have a lone pair of electrons) Such an Oxygen having extra electrons
Percentage of drugs approved in clinical trials
0.01%
Percentage of drug trials that become approved via passing each step?
Less than 10%
What is the Investigational New Drug Application (IND)
A document for drug trials
Phase 1 of drug trials
Tests healthy volunteers (unless for cancer pts, then phase 1 studies pts with cancer)
Absorption, distribution, metabolism, or excretion of drug
Side effects
Dosage and best route of administration determined
Approx. 70% of drugs move to the next phase
Phase 2 of drug trials
Studies efficacy and side effects
Given to pts w/ disease or condition
Provides additional safety data
Approx. 70% of drugs move to next phase
Phase 3 of drug trials
Determine efficacy and monitor adverse reactions
Provides most of the safety data
Common side effects become more present
More likely to determine long-term or rare side effect
Approx 25-30% of drugs move to the next phase
Phase 4 of drug trials
Determine safety and efficacy
Carried out once drug is approved by FDA
define pharmacokinetics
movement of the drug in the body
defined as the study of time course of Absorption, Distribution, Metabolism, and Excretion (ADME) of drugs
define pharmacodynamics
power of the drug in the body
what is Absorption heavily dependent on
route of administration
Distribution
process of drug travelling to numerous locations in the body to and from the blood and various tissues
Metabolism
where drug is modified, usually by specialized enzymatic systems
Metabolism- major site of metabolism?
liver
