Identification

Name
Lanthanum carbonate
Accession Number
DB06792
Type
Small Molecule
Groups
Approved
Description

Lanthanum carbonate is used in medicine as a phosphate binder. As a medication it is sold under the trade name Fosrenol by the pharmaceutical company Shire Pharmaceuticals. Fosrenol is the largest of all pills filled in community pharmacies. Sometimes patients forget that fosrenol is not swallowed whole, but instead should be chewed. This has led to severe choking. It is prescribed for the treatment of hyperphosphatemia, primarily in patients with chronic kidney disease. It is taken with meals and binds to dietary phosphate, preventing phosphate from being absorbed by the intestine.

Structure
Thumb
Synonyms
  • Lanthanum (III) carbonate
  • Lanthanum carbonate anhydrous
  • Lanthanum sesquicarbonate
  • Lanthanum(3+) carbonate
Product Ingredients
IngredientUNIICASInChI Key
Lanthanum carbonate hydrate490D9F069T54451-24-0AFCUGQOTNCVYSW-UHFFFAOYSA-H
Active Moieties
NameKindUNIICASInChI Key
Lanthanum III cationionicO7FU5X12W516096-89-2CZMAIROVPAYCMU-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
FosrenolPowder1000 mg/1OralShire US Manufacturing Inc.2014-09-24Not applicableUs
FosrenolTablet, chewable250 mgOralShire Pharma Canada Ulc2006-12-06Not applicableCanada
FosrenolTablet, chewable500 mg/1OralCardinal Health2004-10-262018-05-15Us
FosrenolTablet, chewable500 mgOralShire Pharma Canada Ulc2006-12-06Not applicableCanada
FosrenolTablet, chewable500 mg/1OralShire US Manufacturing Inc.2004-10-26Not applicableUs
FosrenolTablet, chewable250 mg/1OralShire2004-10-262008-01-31Us
FosrenolTablet, chewable1000 mg/1OralShire US Manufacturing Inc.2005-11-23Not applicableUs
FosrenolTablet, chewable750 mgOralShire Pharma Canada Ulc2006-12-06Not applicableCanada
FosrenolTablet, chewable500 mg/1OralAvera McKennan Hospital2015-03-032018-06-26Us
FosrenolTablet, chewable1000 mgOralShire Pharma Canada Ulc2006-12-06Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Lanthanum CarbonateTablet, chewable500 mg/1OralLupin Pharmaceuticals, Inc.2017-08-30Not applicableUs
Lanthanum CarbonateTablet, chewable1000 mg/1OralLupin Pharmaceuticals, Inc.2017-08-30Not applicableUs
Lanthanum carbonateTablet, chewable750 mg/1OralPrasco Laboratories2017-08-30Not applicableUs
Lanthanum CarbonateTablet, chewable750 mg/1OralLupin Pharmaceuticals, Inc.2017-08-30Not applicableUs
Lanthanum carbonateTablet, chewable500 mg/1OralPrasco Laboratories2017-08-30Not applicableUs
Lanthanum carbonateTablet, chewable1000 mg/1OralPrasco Laboratories2017-08-30Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Lancell SlimmingLanthanum carbonate (2.5 mL/100mL) + Stypocaulon scoparium (2 mL/100mL)GelTopicalMICELLBio Co., Ltd2010-08-19Not applicableUs
International/Other Brands
Foznol / Phosbloc
Categories
UNII
0M78EU4V9H
CAS number
587-26-8
Weight
Average: 457.835
Monoisotopic: 457.76695
Chemical Formula
C3La2O9
InChI Key
NZPIUJUFIFZSPW-UHFFFAOYSA-H
InChI
InChI=1S/3CH2O3.2La/c3*2-1(3)4;;/h3*(H2,2,3,4);;/q;;;2*+3/p-6
IUPAC Name
dilanthanum(3+) ion tricarbonate
SMILES
[La+3].[La+3].[O-]C([O-])=O.[O-]C([O-])=O.[O-]C([O-])=O

Pharmacology

Indication

Used to reduce serum phosphate in patients with end stage renal disease (ESRD).

Associated Conditions
Pharmacodynamics

In vitro studies have shown that lanthanum binds phosphate in the physiologically relevant pH range of 3 to 7. In simulated gastric fluid, lanthanum binds approximately 97% of the available phosphate at pH 3-5 and 67% at pH 7, when lanthanum is present in a two-fold molar excess to phosphate. Bile acids have not been shown to affect the phosphate binding affinity of lanthanum. In order to bind dietary phosphate, lanthanum carbonate must be administered with or immediately after meals.

Mechanism of action

Lanthanum carbonate is a phosphate binder that reduces absorption of phosphate by forming insoluble lanthanum phosphate complexes that pass through the gastrointestinal (GI) tract unabsorbed. Both serum phosphate and calcium phosphate product are reduced as a consequence of the reduced dietary phosphate absorption.

TargetActionsOrganism
APhosphate
binder
Human
Absorption

Bioavailability very low (<0.002%) following single or multiple dose oral administration.

Volume of distribution
Not Available
Protein binding

In vitro, lanthanum is highly bound (>99%) to human plasma proteins, including human serum albumin, α1-acid glycoprotein, and transferrin.

Metabolism

Lanthanum is not metabolized.

Route of elimination

No information is available regarding the mass balance of lanthanum in humans after oral administration. In rats and dogs, the mean recovery of lanthanum after an oral dose was about 99% and 94%, respectively, and was essentially all from feces. Biliary excretion is the predominant route of elimination for circulating lanthanum in rats.

Half life

Elimination half-life of 53 hours.

Clearance

In healthy volunteers administered intravenous lanthanum as the soluble chloride salt (120 μg), renal clearance was less than 2% of total plasma clearance.

Toxicity

The symptoms associated with overdose are adverse reactions such as headache, nausea and vomiting. Lanthanum carbonate was not acutely toxic in animals by the oral route. No deaths and no adverse effects occurred in mice, rats or dogs after single oral doses of 2000 mg/kg.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidThe serum concentration of 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid can be decreased when it is combined with Lanthanum carbonate.
3,5-diiodothyropropionic acidLanthanum carbonate can cause a decrease in the absorption of 3,5-diiodothyropropionic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
AbaloparatideLanthanum carbonate can cause a decrease in the absorption of Abaloparatide resulting in a reduced serum concentration and potentially a decrease in efficacy.
AmpicillinThe serum concentration of Ampicillin can be decreased when it is combined with Lanthanum carbonate.
AtorvastatinThe absorption of Atorvastatin can be decreased when combined with Lanthanum carbonate.
BenazeprilThe serum concentration of Benazepril can be decreased when it is combined with Lanthanum carbonate.
BenazeprilatThe serum concentration of Benazeprilat can be decreased when it is combined with Lanthanum carbonate.
BenzylthiouracilLanthanum carbonate can cause a decrease in the absorption of Benzylthiouracil resulting in a reduced serum concentration and potentially a decrease in efficacy.
CaptoprilThe serum concentration of Captopril can be decreased when it is combined with Lanthanum carbonate.
CarbimazoleLanthanum carbonate can cause a decrease in the absorption of Carbimazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Compound
168924
PubChem Substance
310264888
ChemSpider
147758
ChEMBL
CHEMBL2096647
Drugs.com
Drugs.com Drug Page
Wikipedia
Lanthanum_carbonate
ATC Codes
V03AE03 — Lanthanum carbonate
AHFS Codes
  • 40:18.19 — Phosphate-removing Agents
FDA label
Download (311 KB)
MSDS
Download (122 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableEnd Stage Renal Disease (ESRD)1
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceChronic Renal Failure (CRF)1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedTreatmentCalciphylaxis1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentHyperphosphataemia1
1CompletedTreatmentHyperphosphataemia in Chronic Kidney Disease1
1CompletedTreatmentPharmacology, Clinical1
2CompletedTreatmentChronic Kidney Disease (CKD)1
2CompletedTreatmentDialysis therapy / Hyperphosphataemia1
2CompletedTreatmentHyperphosphataemia / Kidney Diseases1
2CompletedTreatmentKidney Diseases1
2RecruitingTreatmentHyperphosphataemia / Hyperphosphataemia in Chronic Kidney Disease1
3Active Not RecruitingOtherChronic Kidney Disease (CKD)1
3Active Not RecruitingTreatmentHemodialysis Treatment / Hyperphosphataemia1
3CompletedTreatmentChronic Kidney Disease, Stage 51
3CompletedTreatmentChronic Renal Failure (CRF)4
3CompletedTreatmentHyperphosphataemia4
3RecruitingTreatmentCalcium Nephrolithiasis / Secondary Hyperoxaluria1
3TerminatedTreatmentChronic Renal Failure (CRF)1
3Unknown StatusTreatmentChronic Kidney Disease (CKD)1
4CompletedTreatmentChronic Kidney Disease (CKD)1
4CompletedTreatmentChronic Renal Failure (CRF)1
4Enrolling by InvitationTreatmentBone Diseases, Metabolic / Hyperphosphataemia / Renal Insufficiency,Chronic1
4RecruitingTreatmentCardiovascular Disease (CVD) / Chronic Kidney Disease (CKD)1
4TerminatedTreatmentKidney Diseases1
4Unknown StatusTreatmentOther Nonspecific Abnormal Serum Enzyme Levels1
Not AvailableCompletedNot AvailableChronic Kidney Disease (CKD)1
Not AvailableCompletedNot AvailableEnd Stage Renal Disease (ESRD)1
Not AvailableCompletedNot AvailableHyperphosphataemia1
Not AvailableCompletedNot AvailableHyperphosphataemia / Kidney Diseases1
Not AvailableCompletedPreventionChronic Kidney Disease (CKD)2
Not AvailableCompletedPreventionKidney Diseases1
Not AvailableCompletedTreatmentChronic Renal Failure (CRF) / Disorders Associated With Peritoneal Dialysis / End-Stage Renal Disease (ESRD)1
Not AvailableUnknown StatusPreventionMetabolic Bone Disease1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
PowderOral1000 mg/1
PowderOral750 mg/1
Tablet, chewableOral1000 mg
Tablet, chewableOral250 mg
Tablet, chewableOral250 mg/1
Tablet, chewableOral500 mg/1
Tablet, chewableOral500 mg
Tablet, chewableOral750 mg
GelTopical
Tablet, chewableOral1000 mg/1
Tablet, chewableOral750 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5968976No1999-10-192018-10-26Us
US7381428No2008-06-032024-08-26Us
US7465465No2008-12-162024-08-26Us
US8980327No2015-03-172030-12-01Us
US9023397No2015-05-052030-12-01Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityPractically insoluble.FDA Label
Predicted Properties
PropertyValueSource
Water Solubility31.0 mg/mLALOGPS
logP0.65ALOGPS
logP0.25ChemAxon
logS-1.2ALOGPS
pKa (Strongest Acidic)6.05ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area63.19 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity31.17 m3·mol-1ChemAxon
Polarizability3.52 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as organic carbonic acids. These are compounds comprising the carbonic acid functional group.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Organic carbonic acids and derivatives
Sub Class
Organic carbonic acids
Direct Parent
Organic carbonic acids
Alternative Parents
Carbonate salts / Organic salts / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Carbonate salt / Carbonic acid / Organic oxygen compound / Organic oxide / Hydrocarbon derivative / Organic salt / Organooxygen compound / Carbonyl group / Aliphatic acyclic compound
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Small molecule
Organism
Human
Pharmacological action
Yes
Actions
Binder
References
  1. Behets GJ, Verberckmoes SC, D'Haese PC, De Broe ME: Lanthanum carbonate: a new phosphate binder. Curr Opin Nephrol Hypertens. 2004 Jul;13(4):403-9. [PubMed:15199290]

Drug created on September 14, 2010 10:21 / Updated on December 10, 2018 13:39