Lanthanum carbonate

Identification

Summary

Lanthanum carbonate is a phosphate binder indicated for the reduction of serum phosphate in patients with end-stage renal disease.

Brand Names
Fosrenol
Generic Name
Lanthanum carbonate
DrugBank Accession Number
DB06792
Background

Lanthanum carbonate is a phosphate binder marketed under the trade name Fosrenol by Shire Pharmaceuticals. It is a large pill that requires thorough chewing to avoid choking and other gastrointestinal adverse effects. It is used to treat elevated phosphate levels, primarily in patients with chronic kidney disease, by binding to dietary phosphate and preventing its absorption in the intestine.2

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 457.835
Monoisotopic: 457.76695
Chemical Formula
C3La2O9
Synonyms
  • Lanthanum (III) carbonate
  • Lanthanum carbonate anhydrous
  • Lanthanum sesquicarbonate
  • Lanthanum(3+) carbonate

Pharmacology

Indication

Lanthanum carbonate is indicated to reduce serum phosphate in patients with end-stage renal disease (ESRD).2

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofHyperphosphatemia••••••••••••
Contraindications & Blackbox Warnings
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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.2 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.2

In comparison to [sevelemer], another common phosphate binder, lanthanum carbonate is more efficacious in lowering serum phosphate concentrations and effectively managing hyperphosphatemia.1

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.2 Both serum phosphate and calcium phosphate product are reduced as a consequence of the reduced dietary phosphate absorption.

TargetActionsOrganism
APhosphate
binder
Humans
Absorption

The bioavailability of lanthanum carbonate following oral administration is exceedingly low (<0.002%), with a mean Cmax of 1.0 ng/mL and average serum concentration of 0.6 ng/mL.2 The timing of food intake relative to lanthanum administration (during and 30 minutes after food intake) has a negligible effect on the systemic level of lanthanum.2

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.2

Metabolism

Lanthanum does not undergo metabolism.2

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.2 Biliary excretion is the predominant route of elimination for circulating lanthanum in rats.2

Half-life

The elimination half-life of lanthanum in patients undergoing dialysis was 53 hours following discontinuation of therapy.2

Clearance

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

Adverse Effects
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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.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
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.
BenazeprilLanthanum carbonate can cause a decrease in the absorption of Benazepril resulting in a reduced serum concentration and potentially a decrease in efficacy.
CaptoprilLanthanum carbonate can cause a decrease in the absorption of Captopril resulting in a reduced serum concentration and potentially a decrease in efficacy.
CerivastatinThe absorption of Cerivastatin can be decreased when combined with Lanthanum carbonate.
Food Interactions
  • Take with food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Lanthanum carbonate hydrate490D9F069T54451-24-0PKOQIYFBOVTYOH-UHFFFAOYSA-H
Active Moieties
NameKindUNIICASInChI Key
Lanthanum III cationionicO7FU5X12W516096-89-2CZMAIROVPAYCMU-UHFFFAOYSA-N
International/Other Brands
Foznol / Phosbloc
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FosrenolPowder1000 mg/1OralTakeda Pharmaceuticals America, Inc.2014-09-24Not applicableUS flag
FosrenolTablet, chewable750 mg/1OralTakeda Pharmaceuticals America, Inc.2005-11-23Not applicableUS flag
FosrenolTablet, chewable500 mg/1OralTakeda Pharmaceuticals America, Inc.2004-10-26Not applicableUS flag
FosrenolTablet, chewable1000 mgOralTakeda2006-12-062024-07-31Canada flag
FosrenolTablet, chewable500 mg/1OralAvera McKennan Hospital2015-03-032017-05-24US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Lanthanum carbonateTablet, chewable750 mg/1OralTeva Pharmaceuticals USA, Inc.2022-05-25Not applicableUS flag
Lanthanum carbonateTablet, chewable750 mg/1OralCipla USA Inc.2022-01-25Not applicableUS flag
Lanthanum carbonateTablet, chewable500 mg/1OralPrasco Laboratories2017-08-30Not applicableUS flag
Lanthanum CarbonateTablet, chewable1000 mg/1OralLupin Pharmaceuticals, Inc.2017-08-30Not applicableUS flag
Lanthanum carbonateTablet, chewable750 mg/1OralExelan Pharmaceuticals, Inc.2022-01-25Not applicableUS flag

Categories

ATC Codes
V03AE03 — Lanthanum carbonate
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Aliphatic acyclic compound / Carbonate salt / Carbonic acid / Carbonyl group / Hydrocarbon derivative / Organic oxide / Organic oxygen compound / Organic salt / Organooxygen compound
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
0M78EU4V9H
CAS number
587-26-8
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

References

General References
  1. Nain P, Nayak N, Maj MC, Singh RK, Kaur J, Jeong Y, Maity S, Nath R, Hilgers RH, Nauhria S, Nauhria S: Efficacy of Lanthanum Carbonate and Sevelamer Carbonate as Phosphate Binders in Chronic Kidney Disease-A Comparative Clinical Study. Pharmacy (Basel). 2023 Feb 2;11(1):27. doi: 10.3390/pharmacy11010027. [Article]
  2. FDA Approved Drug Products: Fosrenol (lanthanum carbonate) chewable tablets/oral powder for oral use (December 2023) [Link]
PubChem Compound
168924
PubChem Substance
310264888
ChemSpider
147758
RxNav
1311070
ChEMBL
CHEMBL2096647
Drugs.com
Drugs.com Drug Page
Wikipedia
Lanthanum_carbonate
FDA label
Download (311 KB)
MSDS
Download (122 KB)

Clinical Trials

Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package
PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
Not AvailableCompletedNot AvailableChronic Kidney Disease (CKD)1somestatusstop reasonjust information to hide
Not AvailableCompletedNot AvailableEnd Stage Renal Disease (ESRD)1somestatusstop reasonjust information to hide
Not AvailableCompletedNot AvailableHyperphosphataemia3somestatusstop reasonjust information to hide
Not AvailableCompletedNot AvailableHyperphosphataemia / Kidney Diseases1somestatusstop reasonjust information to hide
Not AvailableCompletedPreventionChronic Kidney Disease (CKD)2somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
PowderOral
PowderOral500 mg
PowderOral1000 mg/1
PowderOral750 mg/1
Tablet, chewableOral
Tablet, chewableOral250 mg/1
Tablet, chewableOral500 mg/1
Tablet, chewableOral954 MG
Tablet, chewableOral500 mg
Tablet, chewableOral750 mg
PowderOral1000 MG
PowderOral750 MG
Tablet, chewableOral1000 MG
Tablet, chewableOral250 MG
Tablet, chewableOral1000 mg/1
Tablet, chewableOral750 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5968976No1999-10-192018-10-26US flag
US7381428No2008-06-032024-08-26US flag
US7465465No2008-12-162024-08-26US flag
US8980327No2015-03-172030-12-01US flag
US9023397No2015-05-052030-12-01US flag

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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Kind
Small molecule
Organism
Humans
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. [Article]

Drug created at September 14, 2010 16:21 / Updated at October 03, 2024 07:20