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BIMM118 New Drug Discovery • Design of compounds for a specific biological function (“Rational drug design”) – Synthesis of naturally occurring compounds or structural analogues • Examples: – Levodopa, H2 receptor antagonists, omeprazole – Use of structural information (receptor, enzyme) to develop interacting compounds • Examples: – STI571 (Glevec®): Bcr-Abl specific inhibitor, but high pK => 2 nd generation Bcr-Abl inhibitors are being designed based on the structure of the Bcr-Abl/STI571 complex – Cloning of genes to produce large biologically active peptides • Examples: – Rec. hormones, cytokines; soluble receptor; antibodies
BIMM118 New Drug Discovery • Extremely high cost of new drug development in general restricts it to the province of large pharmaceutical companies • Cost of new drug development is in the $100 to $500 million range • Cost of initial marketing is also very high • Incentives are very high with important new drugs having greater than $1 Billion in yearly sales
Page 1 and 2: BIMM118 “One of the features whic
Page 3 and 4: BIMM118 Definitions • Prophylacti
Page 5 and 6: BIMM118 History of Pharmacology •
Page 11: BIMM118 New Drug Discovery • Synt
Page 15 and 16: BIMM118 Orphan Drugs • Drugs for
Page 17 and 18: BIMM118 Drug Approval Historically,
Page 19 and 20: BIMM118 • Safety Drug Approval -
Page 21 and 22: BIMM118 Drug Efficacy • Efficacy
Page 23 and 24: BIMM118 Drug Efficacy - Dietary Sup
Page 25 and 26: BIMM118 Preclinical Studies • Pha
Page 27 and 28: BIMM118 • Toxicological effects P
Page 29 and 30: BIMM118 • Acute Toxicity Toxicity
Page 31 and 32: BIMM118 • Animal Studies: Toxicit
Page 33 and 34: BIMM118 Phase I Studies • Studies
Page 35 and 36: BIMM118 Phase II Studies • Pharma
Page 37 and 38: BIMM118 Phase III Studies • Rando
Page 39 and 40: BIMM118 Phase IV studies: • Postm
Page 41 and 42: BIMM118 The Four Cornerstones of Ph
Page 43 and 44: BIMM118 Oral Drug Administration
Page 49 and 50: BIMM118 Percutaneous Drug Administr
Page 51 and 52: BIMM118 Percutaneous Drug Administr
Page 53 and 54: BIMM118 Other Topical Drug Administ
Page 55 and 56: BIMM118 • Advantages: - 100% “A
Page 57 and 58: BIMM118 Drug Distribution • To be
Page 59 and 60: BIMM118 • Membrane Permeation: -
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BIMM118 Drug Distribution Volume of
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BIMM118 Clearance (CL) [ml/min]: Dr
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BIMM118 Drug Distribution Dosage Re
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BIMM118 Drug Distribution • Drug
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BIMM118 BLOOD LEVEL TOXIC LEVELS Ma
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BIMM118 • Therapeutic Index: Ther
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BIMM118 Drug Metabolism • Most me
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BIMM118 Drug Metabolism
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BIMM118 Drug Metabolism - Oxidation
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BIMM118 • Drug oxidation requires
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BIMM118 Epoxidation: Dealkylation:
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BIMM118 Azo-reduction: Nitro-reduct
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BIMM118 Drug Metabolism - Phase I
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BIMM118 Drug Metabolism - Glucuroni
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BIMM118 Acetylation: Drug Metabolis
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BIMM118 Drug Metabolism - Phase I &
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BIMM118 Antagonists: Drug Action: R
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BIMM118 Drug Targets
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BIMM118 Drug Targets: Receptors Res
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BIMM118 Receptors • Rapidly actin
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BIMM118 Calcium as Second Messenger
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BIMM118 Three types: Type L N T Cal
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BIMM118 Removal of Ca ++ : • Ca +
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BIMM118 G-Protein-coupled Receptors
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BIMM118 Cyclic Nucleotides - PKA al
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BIMM118 Phosphodiesterases: Cyclic
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BIMM118 Regulation of Receptors •
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BIMM118 Receptor Down-Regulation
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BIMM118 • Examples: Nuclear Recep
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BIMM118 Phospholipids, Phosphoinosi
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BIMM118 • Prostaglandins: Arachid
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BIMM118 • Leukotrienes: Arachidon
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BIMM118 Growth Factor Receptors •
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BIMM118 Signaling through Adapter p
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BIMM118 • “Classical” hormone
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BIMM118 Cytokine Receptors • Curr
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BIMM118 Ser/Thr-kinase Receptors Tr
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BIMM118 NFκB - originally identifi
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BIMM118 Autonomic Nervous System
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BIMM118 Transmitters: • Acetylcho
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BIMM118 Cholinergic receptors: •
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BIMM118 Cholinergic System - Agonis
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BIMM118 Cholinergic System - Antago
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BIMM118 Autonomic Nervous System
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BIMM118 Transmitters: • Acetylcho
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BIMM118 Adrenergic receptors: • a
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BIMM118 Sympathomimetics Adrenergic
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BIMM118 Sympathomimetics Non-select
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BIMM118 Sympathomimetics α 1 - sel
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BIMM118 β 1 - receptors • Mostly
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BIMM118 Sympathomimetics β 2 - sel
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BIMM118 Sympatholytics α 2 - selec
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BIMM118 Sympatholytics β - selecti
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BIMM118 β-Sympatholytics Epinephri
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BIMM118 Cardiovascular Pharmacology
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BIMM118 Potential drug targets: Ant
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BIMM118 Antihypertensive Drugs:Vaso
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BIMM118 Antihypertensive Drugs: Vas
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BIMM118 Antihypertensive Drugs: RAA
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BIMM118 Antihypertensive Drugs: RAA
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BIMM118 • Nitroglycerin - Organic
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BIMM118 Arrhythmias: Cardiac Arrhyt
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BIMM118 Arrhythmias: Cardiac Arrhyt
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BIMM118 Arrhythmias: Other antiarrh
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BIMM118 Congestive Heart Failure Cl
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BIMM118 Cardiac Glycosides: Congest
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BIMM118 Cardiac Glycosides: Congest
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BIMM118 Renal Pharmacology Diuretic
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BIMM118 Functions Renal Pharmacolog
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BIMM118 Diuretics: • Increase out
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BIMM118 Diuretics: Renal Pharmacolo
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BIMM118 Renal Pharmacology Major si
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BIMM118 Diuretics: Osmotic diuretic
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BIMM118 Renal Pharmacology Uric aci
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BIMM118 Gastrointestinal Pharmacolo
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BIMM118 Antacids: Gastrointestinal
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BIMM118 Antacids: Gastrointestinal
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BIMM118 Diabetes mellitus Pancreas:
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BIMM118 Diabetes mellitus
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BIMM118 Diabetis mellitus: Diabetes
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BIMM118 Insulin: Diabetes mellitus
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BIMM118 Insulin: • Insulin Glargi
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BIMM118 Diabetes mellitus Oral hypo
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BIMM118 Diabetes mellitus Oral hypo
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BIMM118 Novel concepts (cont’d):
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BIMM118 Artherosclerosis: Hyperlipi
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BIMM118 Artherosclerosis: Hyperlipi
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BIMM118 Cholesterol: - 60-70% (=100
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BIMM118 Lipid-lowering drugs: Hyper
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BIMM118 Lipid-lowering drugs: Hyper
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BIMM118 Hyperlipidemia
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BIMM118 Adrenal gland: • Medulla:
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BIMM118 Adrenocortical Hormones Ste
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BIMM118 Glucocorticoids (GC): Adren
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BIMM118 Glucocorticoids (GC): • H
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BIMM118 Glucocorticoids (GC): • T
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BIMM118 Steroid-based Drugs • Sex
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BIMM118 Sex Steroids • Female rep
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BIMM118 Sex Steroids • Female rep
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BIMM118 Sex Steroids Estrogens - Es
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BIMM118 Anti-Estrogens • Tamoxife
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BIMM118 Progesterons Sex Steroids T
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BIMM118 Sex Steroids • Male repro
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BIMM118 Androgens Sex Steroids •
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BIMM118 Anabolic Androgens • Dehy
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BIMM118 GnRH analogs/modifiers Sex
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BIMM118 Oral Contraceptives Sex Ste
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BIMM118 Contraceptives Sex Steroids
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BIMM118 Drugs against Allergies •
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BIMM118 Allergy - Symptoms
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BIMM118 Allergy - Food • Allergic
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BIMM118 Latex has cross-reactive ep
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BIMM118 Allergy - Drugs Predominant
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BIMM118 Allergy - Mediators
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BIMM118 Allergy - Histamine Histami
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BIMM118 Allergy - Drugs Targeting H
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BIMM118 H1-Antagonists (“Antihist
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BIMM118 H1-Antagonists (“Antihist
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BIMM118 Mast Cell Stabilizers • C
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BIMM118 Allergy - Leukotrienes Cys-
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BIMM118 Drugs Targeting the CNS •
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BIMM118 Drugs Targeting the CNS Glu
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BIMM118 Dopamine • Inhibitory ami
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BIMM118 Drugs Targeting the CNS Sit
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BIMM118 Hypnotics / Anxiolytics Bar
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BIMM118 Hypnotics / Anxiolytics Ben
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BIMM118 Antidepressants Clinical De
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BIMM118 Tricyclic antidepressants:
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BIMM118 Schizophrenia Endogenous ps
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BIMM118 Classical neuroleptics: Adv
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BIMM118 Pathology: Parkinson’s Di
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BIMM118 Dopamine replacement: Parki
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BIMM118 Pathology: Epilepsy - Group
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BIMM118 Treatment strategies: Inhib
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BIMM118 Ethanol Most widely consume
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BIMM118 Treatment strategies: • D
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BIMM118 General Anesthetics State o
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BIMM118 General Anesthetics Inhalat
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BIMM118 General Anesthetics Intrave
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BIMM118 Opioid Analgesics Opiates:
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BIMM118 Opiates: Mechanism of analg
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BIMM118 Codeine (3-methoxy-morphine
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BIMM118 Meperidine (Pethidine): - A
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BIMM118 Mode of action: Local Anest
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BIMM118 Classification: Local Anest
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BIMM118 Clinical use and Administra
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BIMM118 NSAIDs Non-Steroidal Anti-I
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BIMM118 NSAIDs Non-Steroidal Anti-I
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BIMM118 Chemotherapeutic Agents •
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BIMM118 Antibiotics • Resistance:
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BIMM118 Classification: • Cell wa
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BIMM118 Antibiotics - Cell wall syn
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BIMM118 Antibiotics - Protein synth
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BIMM118 Sulfonamides Antibiotics -
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BIMM118 Quinolones Antibiotics - Qu
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BIMM118 Antibiotics - Summary
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BIMM118 Fungal Growth Patterns •
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BIMM118 Fungal Habitats • Most cl
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BIMM118 Superficial Mycoses • Tin
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BIMM118 • Tinea corporis Cutaneou
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BIMM118 • Sporotrichosis Subcutan
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BIMM118 Systemic Mycosis • Histop
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BIMM118 Opportunistic Mycosis - Som
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BIMM118 Opportunistic Mycosis • C
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BIMM118 Differences between fungi a
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BIMM118 Antifungal Drugs - Polyenes
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BIMM118 Imidazoles • Clotrimazole
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BIMM118 Antifungal Drugs - Azoles T
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BIMM118 Antifungal Drugs - Antimeta
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BIMM118 Antifungal Drugs - Allylami
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