Drug/Small Molecule:
risedronate

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with risedronate that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105238

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all risedronate variant annotations

Gene ? Variant?
(142)
Alternate Names ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA No Variant Annotations available
rs16944 -598T>C, 113594867A>G, 3343530A>G, 4490T>C, IL1B: -511 C/T
A > G
5' Flanking
No VIP available CA No Variant Annotations available
rs2297480 -1-373T>G, -1-98T>G, -175+726T>G, -22-352T>G, 155279482T>G, 6768124T>G
T > G
Intronic
No VIP available No Clinical Annotations available VA
rs3736228 126188C>T, 13507090C>T, 3989C>T, 68201295C>T, Ala1330Val, LRP5: A1330V
C > T
Missense
Ala1330Val
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 142
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • NE-58095
  • Risedronate sodium
  • Risedronic acid
  • risedronate
Trade Names
  • Actonel
  • Actonel 150
  • Benet
Brand Mixture Names

PharmGKB Accession Id:
PA451255

Description

Risedronate is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget's disease of bone.

Source: Drug Bank

Indication

For the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

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.

Source: Drug Bank

Pharmacology

Risedronate is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism and is indicated for the treatment and prevention of osteoporosis in postmenopausal women.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

No evidence found for metabolization of risedronate in humans or mammals

Source: Drug Bank

Protein Binding

~24%

Source: Drug Bank

Absorption

Rapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract

Source: Drug Bank

Half-Life

1.5 hours

Source: Drug Bank

Toxicity

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.

Source: Drug Bank

Clearance

Source: Drug Bank

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.

Source: Drug Bank

Volume of Distribution

  • 13.8 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C7H11NO7P2

Source: Drug Bank

Isomeric SMILES

C1=CC(=CN=C1)CC(O)(P(=O)(O)O)P(=O)(O)O

Source: Drug Bank

OC(CC1=CC=CN=C1)(P(O)(O)=O)P(O)(O)=O

Source: Drug Bank

Canonical SMILES

OC(CC1=CN=CC=C1)(P(O)(O)=O)P(O)(O)=O

Source: Drug Bank

Average Molecular Weight

283.1123

Source: Drug Bank

Monoisotopic Molecular Weight

283.001074735

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

EvidenceGene
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
FDPS
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
IL1B
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
LRP5

Drug Targets

Gene Description
FDPS (source: Drug Bank)

Drug Interactions

Drug Description
risedronate Formation of non-absorbable complexes (source: Drug Bank)
risedronate Formation of non-absorbable complexes (source: Drug Bank)
risedronate Formation of non-absorbable complexes (source: Drug Bank)
risedronate Formation of non-absorbable complexes (source: Drug Bank)
risedronate Formation of non-absorbable complexes (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to risedronate: 6

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The future of pharmacogenetics for osteoporosis. Pharmacogenomics. 2013. Marini Francesca, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Bisphosphonates pathway. Pharmacogenetics and genomics. 2011. Gong Li, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Common allelic variants of the farnesyl diphosphate synthase gene influence the response of osteoporotic women to bisphosphonates. The pharmacogenomics journal. 2010. Olmos J M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
LRP5 Polymorphisms and response to risedronate treatment in osteoporotic men. Calcified tissue international. 2009. Kruk Marcin, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Modulatory effect of farnesyl pyrophosphate synthase (FDPS) rs2297480 polymorphism on the response to long-term amino-bisphosphonate treatment in postmenopausal osteoporosis. Current medical research and opinion. 2008. Marini Francesca, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
-511 C/T IL1B gene polymorphism is associated to resistance to bisphosphonates treatment in Paget disease of bone. Bone. 2006. Corral-Gudino Luis, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0149-0471-01
DrugBank:
DB00884
PDB:
RIS
KEGG Compound:
C08233
PubChem Compound:
5245
PubChem Substance:
46507526
634947
Drugs Product Database (DPD):
2242518
BindingDB:
12576
ChemSpider:
5055
HET:
RIS
Therapeutic Targets Database:
DAP000658
FDA Drug Label at DailyMed:
563c6d6d-56df-43a7-a7aa-709c5ea3cdbe

Clinical Trials

These are trials that mention risedronate and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.