leucovorin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	1232	58-05-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sodium folinate folinic acid leucovorin calcium folinate leucovorin calcium folinic acid calcium salt folinic acid calcium wellcovorin folinic acid calcium salt pentahydrate	The active metabolite of FOLIC ACID. Leucovorin is used principally as an antidote to FOLIC ACID ANTAGONISTS. Molecular weight: 473.45 Formula: C20H23N7O7 CLOGP: -1.98 LIPINSKI: 2 HAC: 14 HDO: 7 TPSA: 215.55 ALOGS: -3.20 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sodium folinate
folinic acid
leucovorin
calcium folinate
leucovorin calcium
folinic acid calcium salt
folinic acid calcium
wellcovorin
folinic acid calcium salt pentahydrate

The active metabolite of FOLIC ACID. Leucovorin is used principally as an antidote to FOLIC ACID ANTAGONISTS.

Molecular weight: 473.45
Formula: C20H23N7O7
CLOGP: -1.98
LIPINSKI: 2
HAC: 14
HDO: 7
TPSA: 215.55
ALOGS: -3.20
ROTB: 9

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
60	mg	O
60	mg	P
60	mg	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	5.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	4 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	100 mg/mL	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	10 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	1.30 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.25 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.09 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
June 20, 1952	FDA
Nov. 25, 2021	PMDA	PFIZER JAPAN INC

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neutropenia	1084.25	11.42	1048	57275	173957	63256742
Neuropathy peripheral	643.72	11.42	649	57674	113018	63317681
Neurotoxicity	495.95	11.42	263	58060	16727	63413972
Mucosal inflammation	450.15	11.42	361	57962	46567	63384132
Thrombocytopenia	438.05	11.42	613	57710	150544	63280155
Disease progression	378.31	11.42	513	57810	122245	63308454
Febrile neutropenia	371.10	11.42	499	57824	117950	63312749
Diarrhoea	341.04	11.42	1426	56897	713940	62716759
Skin toxicity	309.92	11.42	128	58195	4586	63426113
Dermatitis acneiform	225.22	11.42	104	58219	4892	63425807

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neutropenia	978.39	12.76	1328	64117	155450	34736036
Skin toxicity	752.50	12.76	297	65148	4487	34886999
Neuropathy peripheral	654.36	12.76	792	64653	82471	34809015
Diarrhoea	535.20	12.76	1769	63676	388143	34503343
Disease progression	458.51	12.76	766	64679	107311	34784175
Dermatitis acneiform	445.45	12.76	222	65223	5967	34885519
Neurotoxicity	420.97	12.76	314	65131	17696	34873790
Mucosal inflammation	413.50	12.76	432	65013	38190	34853296
Metastases to liver	332.26	12.76	244	65201	13419	34878067
Thrombocytopenia	326.15	12.76	826	64619	155421	34736065

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neutropenia	2017.62	11.12	2242	109839	285468	79346839
Neuropathy peripheral	1449.60	11.12	1354	110727	139951	79492356
Skin toxicity	983.35	11.12	388	111693	7926	79624381
Disease progression	913.24	11.12	1207	110874	183155	79449152
Neurotoxicity	862.60	11.12	549	111532	31969	79600338
Mucosal inflammation	810.26	11.12	743	111338	74837	79557470
Diarrhoea	764.10	11.12	2835	109246	877654	78754653
Thrombocytopenia	756.47	11.12	1344	110737	263915	79368392
Dermatitis acneiform	639.00	11.12	302	111779	9691	79622616
Polyneuropathy	498.68	11.12	349	111732	23802	79608505

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	V03AF03	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Detoxifying agents for antineoplastic treatment
ATC	V03AF06	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Detoxifying agents for antineoplastic treatment
CHEBI has role	CHEBI:75771	Mus musculus metabolites
CHEBI has role	CHEBI:76971	Escherichia coli metabolites
FDA CS	M0008658	Folic Acid
FDA EPC	N0000178369	Folate Analog
MeSH PA	D000931	Antidotes
MeSH PA	D018977	Micronutrients
MeSH PA	D020011	Protective Agents
MeSH PA	D014803	Vitamin B Complex

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Megaloblastic anemia	indication	53165003	DOID:13382
Folic acid deficiency	indication	190633005
Bone Marrow Suppression due to Folic Acid Antagonism	indication
Methotrexate Toxicity	indication
Trimethoprim Toxicity	indication
Trimetrexate Toxicity	indication
Sulfadiazine Toxicity	indication
Pyrimethamine Toxicity	indication
Adjunct to Fluorouracil Treatment of Colorectal Cancer	indication
Pernicious anemia	contraindication	84027009	DOID:13381

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.61	acidic
pKa2	5.29	acidic
pKa3	10.26	acidic
pKa4	12.96	acidic
pKa5	4.59	Basic
pKa6	2.23	Basic

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Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Thymidylate synthase	Enzyme	P04818	TYSY_HUMAN		Ki	4.07		WOMBAT-PK
Dihydrofolate reductase	Enzyme	P00374	DYR_HUMAN		Ki	5.63		CHEMBL

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External reference:

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ID	Source
001050	NDDF
001051	NDDF
009520	NDDF
126223008	SNOMEDCT_US
135403648	PUBCHEM_CID
1492-18-8	SECONDARY_CAS_RN
1528001	SNOMEDCT_US
1728	MMSL
225852	RXNORM
396065004	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0054-4496	TABLET	5 mg	ORAL	ANDA	15 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0054-4497	TABLET	10 mg	ORAL	ANDA	15 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0054-4498	TABLET	15 mg	ORAL	ANDA	15 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0054-4499	TABLET	25 mg	ORAL	ANDA	15 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0054-8496	TABLET	5 mg	ORAL	ANDA	15 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9368	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAMUSCULAR	ANDA	19 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9368	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAMUSCULAR	ANDA	19 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9552	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	350 mg	INTRAMUSCULAR	ANDA	19 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9553	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAMUSCULAR	ANDA	19 sections
Leucovorin Calcium	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9554	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	100 mg	INTRAMUSCULAR	ANDA	19 sections

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