Details of the Drug

General Information of Drug (ID: DM5FLTY)

Drug Name

Risedronate

Synonyms

Risedronic acid; 105462-24-6; Actonel; Atelvia; Acido risedronico; Acidum risedronicum; Benet; Risedronic acid [INN:BAN]; Acidum risedronicum [INN-Latin]; Acido risedronico [INN-Spanish]; Acide risedronique [INN-French]; Risedronic acid monohydrate; NE-58095; UNII-KM2Z91756Z; C7H11NO7P2; NE 58019; HSDB 7326; [1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethyl]phosphonic acid; (1-hydroxy-1-phosphono-2-pyridin-3-yl-ethyl)phosphonic acid; Risedronic acid (Actonel); CHEMBL923; CHEBI:8869; Phosphonic acid,; Benet; RIS; Ridron; Acide risedronique; Bisphosphonate 1; Actonel (TN); Ridron (TN); Risedronic acid (INN); (1-Hydroxy-2-(3-pyridyl)ethylidene)diphosphonic acid; (1-hydroxy-1-phosphono-2-pyridin-3-ylethyl)phosphonic acid; (1-hydroxy-2-pyridin-3-ylethane-1,1-diyl)bis(phosphonic acid); 1-HYDROXY-2-(3-PYRIDINYL)ETHYLIDENE BIS-PHOSPHONIC ACID

Indication

Disease Entry	ICD 11	Status	REF
Paget's disease	FB85	Approved	[1], [2]

Therapeutic Class

Bone Density Conservation Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 1

Molecular Weight (mw)

283.11

Topological Polar Surface Area (xlogp)

-3.1

Rotatable Bond Count (rotbonds)

4

Hydrogen Bond Donor Count (hbonddonor)

5

Hydrogen Bond Acceptor Count (hbondacc)

8

ADMET Property

Absorption Tmax: The time to maximum plasma concentration (Tmax) is 20-40 min [3]
Clearance: The renal clearance of drug is 52 mL/min [4]
Half-life: The concentration or amount of drug in body reduced by one-half in 1.5 hours [5]
Metabolism: The drug is not metabolised [6]
Vd: The volume of distribution (Vd) of drug is 13.8 L/kg [4]

Chemical Identifiers

Formula: C7H11NO7P2
IUPAC Name: (1-hydroxy-1-phosphono-2-pyridin-3-ylethyl)phosphonic acid
Canonical SMILES: C1=CC(=CN=C1)CC(O)(P(=O)(O)O)P(=O)(O)O
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)
InChIKey: IIDJRNMFWXDHID-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 5245
ChEBI ID: CHEBI:8869
CAS Number: 105462-24-6
DrugBank ID: DB00884
TTD ID: D0PA5S
ACDINA ID: D00598

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Geranyltranstransferase (FDPS)	TTIKWV4	FPPS_HUMAN	Inhibitor	[7], [8]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Molecular Expression Atlas of This Drug

The Studied Disease

Paget's disease

ICD Disease Classification

FB85

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Geranyltranstransferase (FDPS)	DTT	FDPS	7.06E-03	-0.73	-2.57

Molecular Expression Atlas (MEA)

MEA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Risedronate (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Framycetin	DMF8DNE	Moderate	Increased risk of hypocalcemia by the combination of Risedronate and Framycetin.	Alcoholic liver disease [DB94]	[16]
Kanamycin	DM2DMPO	Moderate	Increased risk of hypocalcemia by the combination of Risedronate and Kanamycin.	Bacterial infection [1A00-1C4Z]	[16]
Streptomycin	DME1LQN	Moderate	Increased risk of hypocalcemia by the combination of Risedronate and Streptomycin.	Bacterial infection [1A00-1C4Z]	[16]
Netilmicin	DMRD1QK	Moderate	Increased risk of hypocalcemia by the combination of Risedronate and Netilmicin.	Bacterial infection [1A00-1C4Z]	[16]
Ketoprofen	DMRKXPT	Moderate	Increased risk of GI mucosal injury/bleeding risk by the combination of Risedronate and Ketoprofen.	Chronic pain [MG30]	[17]
Ethacrynic acid	DM60QMR	Moderate	Increased risk of hypocalcemia by the combination of Risedronate and Ethacrynic acid.	Essential hypertension [BA00]	[18]
Bumetanide	DMRV7H0	Moderate	Increased risk of hypocalcemia by the combination of Risedronate and Bumetanide.	Heart failure [BD10-BD1Z]	[18]
Didanosine	DMI2QPE	Moderate	Decreased absorption of Risedronate due to formation of complexes caused by Didanosine.	Human immunodeficiency virus disease [1C60-1C62]	[19]
Etelcalcetide	DMHP9BL	Major	Increased risk of hypocalcemia by the combination of Risedronate and Etelcalcetide.	Hyper-parathyroidism [5A51]	[20]
Meclofenamic acid	DM05FXR	Moderate	Increased risk of nephrotoxicity by the combination of Risedronate and Meclofenamic acid.	Inflammatory spondyloarthritis [FA92]	[17]
Iron	DMAP8MV	Moderate	Decreased absorption of Risedronate due to formation of complexes caused by Iron.	Iron deficiency anaemia [3A00]	[19]
Exjade	DMHPRWG	Major	Increased risk of GI mucosal injury/bleeding risk by the combination of Risedronate and Exjade.	Mineral absorption/transport disorder [5C64]	[21]
Lanthanum carbonate	DMMJQSH	Moderate	Decreased absorption of Risedronate due to formation of complexes caused by Lanthanum carbonate.	Mineral absorption/transport disorder [5C64]	[22]
Aspirin	DM672AH	Moderate	Increased risk of nephrotoxicity by the combination of Risedronate and Aspirin.	Pain [MG30-MG3Z]	[17]
Ibuprofen	DM8VCBE	Moderate	Increased risk of nephrotoxicity by the combination of Risedronate and Ibuprofen.	Pain [MG30-MG3Z]	[17]
Choline salicylate	DM8P137	Moderate	Increased risk of GI mucosal injury/bleeding risk by the combination of Risedronate and Choline salicylate.	Postoperative inflammation [1A00-CA43]	[17]
Bromfenac	DMKB79O	Moderate	Increased risk of nephrotoxicity by the combination of Risedronate and Bromfenac.	Postoperative inflammation [1A00-CA43]	[17]
Salsalate	DM13P4C	Moderate	Increased risk of GI mucosal injury/bleeding risk by the combination of Risedronate and Salsalate.	Rheumatoid arthritis [FA20]	[17]
Oxaprozin	DM9UB0P	Moderate	Increased risk of nephrotoxicity by the combination of Risedronate and Oxaprozin.	Rheumatoid arthritis [FA20]	[17]
Salicyclic acid	DM2F8XZ	Moderate	Increased risk of nephrotoxicity by the combination of Risedronate and Salicyclic acid.	Seborrhoeic dermatitis [EA81]	[17]
Plazomicin	DMKMBES	Moderate	Increased risk of hypocalcemia by the combination of Risedronate and Plazomicin.	Urinary tract infection [GC08]	[16]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
FD&C blue no. 2	E00446	2723854	Colorant
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Quinoline yellow WS	E00309	24671	Colorant
Sodium stearyl fumarate	E00545	23665634	lubricant
Sunset yellow FCF	E00255	17730	Colorant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Crospovidone	E00626	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Hypromellose	E00634	Not Available	Coating agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 3350	E00652	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 400	E00653	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium phosphate monobasic monohydrate	E00428	516949	Buffering agent; Complexing agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triacetin	E00080	5541	Humectant; Plasticizing agent; Solvent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Risedronic acid 5 mg tablet	5 mg	Oral Tablet	Oral
Risedronic acid 150 mg tablet	150 mg	Oral Tablet	Oral
Risedronic acid 30 mg tablet	30 mg	Oral Tablet	Oral
Risedronic acid 35 mg tablet	35 mg	Oral Tablet	Oral
Risedronic acid 75 mg tablet	75 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3176).
2	Risedronate for treatment of osteoporosis. Nippon Rinsho. 2009 May;67(5):948-53.
3	FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
4	An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9.
5	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6	Ghannoum M, Arendrup MC, Chaturvedi VP, Lockhart SR, McCormick TS, Chaturvedi S, Berkow EL, Juneja D, Tarai B, Azie N, Angulo D, Walsh TJ: Ibrexafungerp: A Novel Oral Triterpenoid Antifungal in Development for the Treatment of Candida auris Infections. Antibiotics (Basel). 2020 Aug 25;9(9). pii: antibiotics9090539. doi: 10.3390/antibiotics9090539.
7	Activity of bisphosphonates against Trypanosoma brucei rhodesiense. J Med Chem. 2002 Jul 4;45(14):2904-14.
8	In vivo activities of farnesyl pyrophosphate synthase inhibitors against Leishmania donovani and Toxoplasma gondii. Antimicrob Agents Chemother. 2002 Mar;46(3):929-31.
9	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10	Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid. J Med Chem. 2010 May 13;53(9):3454-64.
11	Detection of nonsterol isoprenoids by HPLC-MS/MS. Anal Biochem. 2008 Dec 1;383(1):18-24.
12	Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther. 2001 Feb;296(2):235-42.
13	Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of hu... J Med Chem. 2008 Apr 10;51(7):2187-95.
14	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
15	The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
16	Chang JT, Green L, Beitz J "Renal failure with the use of zoledronic acid." N Engl J Med 349 (2003): 1676-9 discussion 1676-9. [PMID: 14573746]
17	Product Information. Actonel (risedronate). Procter and Gamble Pharmaceuticals, Cincinnati, OH.
18	Product Information. Skelid (tilundronate). Sanofi Winthrop Pharmaceuticals, New York, NY.
19	Product Information. Bonefos (clodronate). Rhone-Poulenc Rorer Canada Inc, Laval, QC.
20	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
21	Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
22	Canadian Pharmacists Association.