Classification of pharmacodynamic targets
Pharmacodynamics examines how drugs exert their effects in the body and the molecular or physicochemical mechanisms through which they modify its function.
Drug targets are most commonly proteins, but nucleic acids, components of pathogens and nonspecific chemical or physical interactions may also contribute to drug effects.
| Main category | Target group | Target type | Specific target or mechanism | Example drug |
|---|---|---|---|---|
| Proteins | Ion channel | Voltage-gated ion channel | Voltage-gated Na⁺ channel | Lidocaine |
| L-type Ca²⁺ channel | Amlodipine | |||
| Enzyme | Catalytic protein | Angiotensin-converting enzyme (ACE) | Ramipril | |
| Cyclooxygenase enzymes (COX) | Ibuprofen | |||
| Monoamine oxidase B (MAO-B) | Selegiline | |||
| Neprilysin | Sacubitril | |||
| Transport protein and pump | Membrane transporter | Serotonin transporter (SERT) | Fluoxetine | |
| Sodium–glucose cotransporter 2 (SGLT2) | Remogliflozin | |||
| Ion pump | Gastric H⁺/K⁺-ATPase proton pump | Pantoprazol | ||
| Na⁺/K⁺-ATPase | Digitoxin | |||
| Receptor | Ion channel receptor | GABAA receptor, ligand-gated Cl⁻ channel | Diazepam | |
| NMDA receptor, ligand-gated cation channel | Memantine | |||
| Intracellular ryanodine receptor, a Ca²⁺-release channel of the endoplasmic reticulum | Dantrolene | |||
| Enzyme-linked receptor | Receptor tyrosine kinase: epidermal growth factor receptor (EGFR) | Erlotinib | ||
| Receptor tyrosine kinase: anaplastic lymphoma kinase (ALK) | Crizotinib | |||
| Receptor serine/threonine kinase: TGF-β type I receptor (TGFBR1/ALK5) | Galunisertib* | |||
| Receptor-associated cytoplasmic tyrosine kinase: cytokine receptor–JAK1/JAK2 signalling | Ruxolitinib | |||
| Membrane-bound receptor guanylyl cyclase: natriuretic peptide receptor A (NPR-A) | Nesiritide | |||
| Receptor tyrosine kinase: insulin receptor | Insulin | |||
| G protein-coupled receptor | Gs-coupled β2-adrenoceptor | Salbutamol | ||
| Gq-coupled M3 muscarinic receptor | Oxybutynin | |||
| Gi-coupled α2-adrenoceptor | Clonidine | |||
| Nuclear receptor | Oestrogen receptor | Tamoxifen | ||
| Vitamin D receptor (VDR) | Calcitriol | |||
| Retinoic acid receptor (RAR) | Retinoic acid | |||
| Thyroid hormone receptor (TR) | Thyroxine (T4; mainly after conversion to T3) | |||
| Structural protein | Cytoskeletal component | Tubulin, the building block of microtubules | Vincristine | |
| Other macromolecule | Nucleic acid | DNA | Formation of DNA crosslinks | Cisplatin |
| Formation of DNA strand breaks | Bleomycin | |||
| Physicochemical and nonspecific effects | Acid–base reaction | Antacid | Chemical neutralisation of gastric acid | Magnesium hydroxide |
| Binding in the intestine | Bile acid-binding resin | Binding of bile acids in the intestine | Colestyramine | |
| Biological neutralisation | Antitoxin | Neutralisation of a bacterial toxin | Tetanus antitoxin | |
| Complex formation | Chelating agent | Binding of heavy metal ions | Dimercaprol | |
| Physical contrast effect | Diagnostic contrast agent | X-ray absorption | Barium sulfate | |
| Targets associated with pathogens | Bacterium | Enzyme | DNA gyrase and topoisomerase IV | Ciprofloxacin |
| Virus | Enzyme | HIV reverse transcriptase | Efavirenz | |
| Fungus | Biosynthetic enzyme system | Ergosterol biosynthesis (lanosterol 14α-demethylase, CYP51) | Fluconazole | |
| Protozoan | Enzyme | Plasmodium falciparum dihydrofolate reductase | Pyrimethamine | |
| Helminth | Ion channel | Glutamate-gated Cl⁻ channel | Ivermectin |
* Galunisertib is an investigational compound; it is included as an example of the pharmacological modulation of a receptor serine/threonine kinase.
Sacubitril does not act directly on a receptor guanylyl cyclase. Through neprilysin inhibition, it increases the concentrations of natriuretic peptides, among others, which can then activate the corresponding receptor guanylyl cyclases.