1.0 2009-07-15 20:44:10 UTC 2026-05-14 16:51:37 UTC T3D2668 Risedronate SmallMolecule Risedronate belongs to the bisphosphonates, a subclass of organic phosphonic acids and derivatives within the organic compounds. It is an exogenous solid with the formula C7H11NO7P2 and an average molecular weight of 283.11 g/mol. This biological drug (PMC10692760, PMC8713161) is administered via the oral exposure route and is used in healthcare, pharmaceuticals, and veterinary products for the treatment of bone diseases. The compound targets geranylgeranyl pyrophosphate synthase (GGPS1) and farnesyl pyrophosphate (FPP) synthase. The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. As a nitrogen-containing bisphosphonate, risedronate acts as an analogue of isoprenoid diphosphate lipids to inhibit FPP synthase, an enzyme in the mevalonate pathway. This inhibition in osteoclasts prevents the biosynthesis of isoprenoid lipids, thereby inhibiting osteoclast activity and reducing bone resorption and turnover. Risedronate is used as a treatment for osteoporosis (PMC10547673, PMC10889292, PMC11012270, PMC2686344, PMC2971711, PMC3010171, PMC3079953), hypercalcemia (PMC10547673), multiple myeloma (PMC10547673), and glucocorticoid-induced osteoporosis (PMC5114204, PMC6924235). It has a therapeutic effect on breast cancer (PMC6607035) and glucocorticoid-induced osteoporosis (PMC2686344). Associated health effects include nausea (PMC2879572), headache (PMC6924235), and an increase in fever (PMC2971711), while it is associated with a decrease in necrosis (PMC10871045) and esophageal cancer (PMC10871045). Drug Synthetic Toxin Organic Compound Drug Calcium Channel Blocker Antihypocalcemic Agent Bisphosphonate Bone Density Conservation Agent Antiresorptive Metabolite Synthetic Compound Acide risédroniqe Acido risedronico Acidum risedronicum Actonel Atelvia Benet NE-58095 Ridron Risedronic acid Risedronsäure C7H11NO7P2 283.1123 283.001074735 [1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethyl]phosphonic acid risedronate 105462-24-6 OC(CC1=CN=CC=C1)(P(O)(O)=O)P(O)(O)=O InChI=1S/C7H11NO7P2/c9-7(16(10,11)12,17(13,14)15)4-6-2-1-3-8-5-6/h1-3,5,9H,4H2,(H2,10,11,12)(H2,13,14,15) IIDJRNMFWXDHID-UHFFFAOYSA-N Organic compounds Organic acids and derivatives Organic phosphonic acids and derivatives Bisphosphonates Bisphosphonates Azacyclic compounds Heteroaromatic compounds Hydrocarbon derivatives Organic oxides Organic phosphonic acids Organonitrogen compounds Organooxygen compounds Organophosphorus compounds Organopnictogen compounds Pyridines and derivatives Aromatic heteromonocyclic compound Azacycle Bisphosphonate Heteroaromatic compound Hydrocarbon derivative Organic nitrogen compound Organic oxide Organic oxygen compound Organoheterocyclic compound Organonitrogen compound Organooxygen compound Organophosphonic acid Organophosphorus compound Organopnictogen compound Pyridine Aromatic heteromonocyclic compounds pyridines Detected and Not Quantified Exogenous Cytoplasm Membrane Risedronate Pathway Risedronate Action Pathway SMP0000112 Risedronate Action Pathway (new) SMP0126323 Risedronate Drug Metabolism Pathway SMP0145445 Solid White powder. solubility 1.04e+01 g/L logp -3.6 logp -0.75 ALOGPS logs -1.43 ALOGPS solubility 1.04e+01 g/l ALOGPS logp -3.3 ChemAxon pka_strongest_acidic 0.68 ChemAxon pka_strongest_basic 4.91 ChemAxon iupac [1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethyl]phosphonic acid ChemAxon average_mass 283.1123 ChemAxon mono_mass 283.001074735 ChemAxon smiles OC(CC1=CN=CC=C1)(P(O)(O)=O)P(O)(O)=O ChemAxon formula C7H11NO7P2 ChemAxon inchi InChI=1S/C7H11NO7P2/c9-7(16(10,11)12,17(13,14)15)4-6-2-1-3-8-5-6/h1-3,5,9H,4H2,(H2,10,11,12)(H2,13,14,15) ChemAxon inchikey IIDJRNMFWXDHID-UHFFFAOYSA-N ChemAxon polar_surface_area 148.18 ChemAxon refractivity 57.12 ChemAxon polarizability 21.91 ChemAxon rotatable_bond_count 4 ChemAxon acceptor_count 8 ChemAxon donor_count 5 ChemAxon physiological_charge -2 ChemAxon formal_charge 0 ChemAxon Rapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass. No evidence found for metabolization of risedronate in humans or mammals. Route of Elimination: Risedronate is excreted unchanged primarily via the kidney. Insignificant amounts (<0.1% of intravenous dose) of drug are excreted in the bile in rats. Half Life: 1.5 hours No indication of carcinogenicity to humans (not listed by IARC). For the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis #<HealthEffect::ActiveRecord_Associations_CollectionProxy:0x00007f722470aa10> Side effects include abdominal pain, anxiety, back pain, belching, bladder irritation, bone disorders and pain, bronchitis, bursitis, cataracts, chest pain, colitis, constipation, depression, diarrhea, difficulty breathing, dizziness, dry eyes, eye infection, flu-like symptoms, gas, headache, high blood pressure, infection, insomnia, itching, joint disorders and pain, leg cramps, muscle pain, muscle weakness, nausea, neck pain, nerve pain, pain, pneumonia, rash, ringing in ears, sinus problems, sore throat, stomach bleeding, stuffy or runny nose, swelling, tendon problems, tumor, ulcers, urinary tract infection, vertigo, vision problems, and weakness. DB00884 HMDB15022 5245 CHEMBL923 5055 C08233 183772 RISEDRONATE Risedronic acid RIS Risedronate 18048412 Drugs.com: http://www.drugs.com/cons/Risedronate.html BE0000776 The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass. Inhibitory 0.00036 uM BindingDB 12576 Inhibitory 0.0822 uM BindingDB 12576 IC50 0.0057 uM BindingDB 12576 IC50 0.01 uM BindingDB 12576 IC50 0.011 uM BindingDB 12576 IC50 0.17 uM BindingDB 12576 IC50 0.3 uM BindingDB 12576 IC50 0.4529 uM BindingDB 12576 IC50 0.86 uM BindingDB 12576 BE0003570 Inhibitory 8300 uM BindingDB 12576 IC50 300 uM BindingDB 12576 IC50 331.13 uM BindingDB 12576 IC50 350 uM BindingDB 12576 BE0004801