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Medicinal Chem
| Question | Answer |
|---|---|
| Medicinal chemistry | Discovering and developing new drugs |
| Pharmaceutical chemistry | Formulation of the drug, preparation, and manufacture of drugs |
| 4 stages in Medicinal chemistry | 1. Drug discovering 2. Preclinical development (large scale synthesis) 3. Clinical Trials 4. FDA review |
| Phase 1 of clinical trials | Healthy volunteers |
| Phase 2 of clinical trials | -Looking for efficacy and what dose -Disease state |
| Phase 3 of clinical trials | Widespread populations to prove efficacy |
| NDA | New drug application |
| IND | Investigational new drug application |
| Patent life | 20 years from date of filling |
| Process it takes to find a drug | 10-17 years |
| How many molecules to get 10 molecules in clinical drugs | 10,000 molecules |
| Average cost of pharmaceutical drug | ~2.6 billion |
| Average cost of Biologic drug | ~1.2 billion |
| Process it takes to develop biologic | ~12 years |
| Biologics License Application | Needed for biologic meds |
| Screen | Assay that measures the activity agent or drug |
| Hit | desired activity in the screen (<10 millimolars) |
| Hit series | Group of structurally related compounds that have the desired activity |
| Lead | Molecule that has therapeutically useful activity (usually nanomolars) |
| Clinical Candidate | molecule expected to be useful for treating human disease |
| Series of medicinal chemistry | target, assay, screening, hit, hit series, lead, clinical candidate |
| target | enzyme, receptor, or other molecule structure that drug interacts with |
| Different ways to target identify | -Phenotypic -Genotypic |
| High throughput screening | -Testing large numbers of compounds for activity in a particular biological target in a short amount of time -Goals to find hits (usually <10 nanomolars) |
| Read-out | result of assay |
| Rational drug design | Involves computer (in silico) modeling |
| Medicinal chemistry | modifying chemical structure of a hit through synthesis, adding different function groups or changing stereochemistry |
| 2 different categories of Rational drug design | -Structure-based drug design -Ligand-based drug design |
| Structure-based drug design | Take crystal structure of either a target protein or a known ligand bound to a target protein from x-ray crystallography |
| Ligand-base drug design | Use a molecule that binds to the target and change the composition of the molecule to find optimal binding and in vivo characteristics |
| On-target effects | -effects caused by binding the intended target protein -both beneficial and adverse |
| off-target effects | -effects caused by binding to a different target or targets than intended -can be both beneficial and adverse |
| Configuration based notation with racemic mix | -Rac- or RS- -R- or S- (found in brand name) -Ar- or Es- (found in generic) |
| Optical rotation-based notation | -Dextro or Levo- -Dex or Lev- -+ or - (found in chemical name) |
| Configuration based by analogy to glyceraldehyde | -D- or L- (found in chemical name-- not as common) |
| Importance of Stereochemistry | -Efficacy or potency -PK properties -toxic effects -cost -increase patent coverage |
| Geometric isomers | Restricted rotation around a bond that produces stereoisomers |
| Bioisosteres | different functional group, roughly the same shape, produces the same effect |
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5917076888326220