Leucovorin
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1952
- First approval year
- 1952
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Leucovorin
- Molecular weight
- 473.45
- Structure (SMILES)
- Nc1nc(=O)c2c([nH]1)NCC(CNc1ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)O)cc1)N2C=O
- 5 formyltetrahydrofolate
- 5 formyltetrahydrofolic acid
- 5-formyltetrahydrofolate
- 5-formyltetrahydrofolic acid
- folinic acid
- Folinic acid
- FOLINIC ACID [MART.]
- FOLINIC ACID [MI]
- Folinic acid [WHO-DD]
- folinic acid mart
- folinic acid mi
- folinic acid who dd
- l glutamic acid n 4 2 amino 5 formyl 1 4 5 6 7 8 hexahydro 4 oxo 6 pteridinyl methyl amino benzoyl
- L-GLUTAMIC ACID, N-(4-(((2-AMINO-5-FORMYL-1,4,5,6,7,8-HEXAHYDRO-4-OXO-6-PTERIDINYL)METHYL)AMINO)BENZOYL)-
- leucovorin
- Leucovorin
- LEUCOVORIN [HSDB]
- LEUCOVORIN [VANDF]
- leucovorin hsdb
- leucovorin vandf
- n p 6rs 2 amino 5 formyl 5 6 7 8 tetrahydro 4 hydroxy 6 pteridinyl methyl amino benzoyl l glutamate
- N-(P-((((6RS)-2-AMINO-5-FORMYL-5,6,7,8-TETRAHYDRO-4-HYDROXY-6-PTERIDINYL)METHYL)AMINO)BENZOYL)-L-GLUTAMATE
- CAS registry numbers
- 58-05-9
- ChEMBL ID
- CHEMBL1679
- InChIKey
- VVIAGPKUTFNRDU-ABLWVSNPSA-N
- PubChem compound IDs
- 135403648
- RxNorm IDs (RxCUI)
- 6313
- FDA ingredient codes (UNII)
- Q573I9DVLP
- Applicant
- HIKMA
- Approval date
- 14 Sept 1987
- Application number
- ANDA089384
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- folinic acid
- Type
- Synthetic organic
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000178
- Subject identifier
- D013274
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Adenocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000228
- Subject identifier
- D000230
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000503
- Subject identifier
- D013274
- Condition
- Glioblastoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Osteosarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000637
- Subject identifier
- D012516
- Condition
- Arthritis, Rheumatoid
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000685
- Subject identifier
- D001172
- Condition
- Down Syndrome
- Highest recorded phase
- 3
- Condition identifier
- EFO:0001064
- Subject identifier
- D004314
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Child Development Disorders, Pervasive
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003756
- Subject identifier
- D002659
- Condition
- Asperger Syndrome
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003757
- Subject identifier
- D020817
- Condition
- Autistic Disorder
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003758
- Subject identifier
- D001321
- Condition
- Uterine Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003859
- Subject identifier
- D014594
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003860
- Subject identifier
- D010190
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003897
- Subject identifier
- D013274
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0004142
- Subject identifier
- D015179
- Condition
- Psychotic Disorders
- Highest recorded phase
- 3
- Condition identifier
- EFO:0005407
- Subject identifier
- D011618
- Condition
- Esophageal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005922
- Subject identifier
- D004938
- Condition
- Biliary Tract Diseases
- Highest recorded phase
- 2
- Condition identifier
- EFO:0009534
- Subject identifier
- D001660
- Condition
- Neoplasm Metastasis
- Highest recorded phase
- 1
- Condition identifier
- EFO:0009708
- Subject identifier
- D009362
- Condition
- Rectal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:1000657
- Subject identifier
- D012004
- Condition
- Colonic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001950
- Subject identifier
- D003110
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001951
- Subject identifier
- D015179
And 13 more, listed on the interactive page.
- Condition identifier
- EFO_0000182
- Condition identifier
- EFO_0000365
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000519
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000574
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 2
- Condition identifier
- EFO_0001064
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003756
- Condition identifier
- EFO_0003859
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003860
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003863
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003897
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004142
- Highest recorded phase
- 3
- Condition identifier
- EFO_0005221
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005407
- Highest recorded phase
- 3
- Condition identifier
- EFO_0005922
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009534
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009708
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000044
- Highest recorded phase
- 3
- Condition identifier
- EFO_1000657
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001480
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001950
- Condition identifier
- HP_0001249
- Highest recorded phase
- 2
- Condition identifier
- HP_0002014
- Condition identifier
- HP_0002894
- Highest recorded phase
- 2
And 85 more, listed on the interactive page.
- Event
- abdominal discomfort
- Reports
- 2,494
- Reporting signal score
- 5,746.55
- Event
- alopecia
- Reports
- 2,672
- Reporting signal score
- 6,312.81
- Event
- anaemia
- Reports
- 347
- Reporting signal score
- 153.354
- Event
- anti-cyclic citrullinated peptide antibody positive
- Reports
- 990
- Reporting signal score
- 4,334.24
- Event
- arthralgia
- Reports
- 932
- Reporting signal score
- 412.311
- Event
- arthropathy
- Reports
- 1,483
- Reporting signal score
- 3,660.11
- Event
- blister
- Reports
- 464
- Reporting signal score
- 681.097
- Event
- blood cholesterol increased
- Reports
- 219
- Reporting signal score
- 233.075
- Event
- colorectal cancer metastatic
- Reports
- 64
- Reporting signal score
- 227.716
- Event
- condition aggravated
- Reports
- 1,089
- Reporting signal score
- 782.505
- Event
- contusion
- Reports
- 296
- Reporting signal score
- 204.667
- Event
- dermatitis acneiform
- Reports
- 120
- Reporting signal score
- 231.991
- Event
- diarrhoea
- Reports
- 1,313
- Reporting signal score
- 401.924
- Event
- discomfort
- Reports
- 1,283
- Reporting signal score
- 3,462.75
- Event
- disease progression
- Reports
- 532
- Reporting signal score
- 456.319
- Event
- drug intolerance
- Reports
- 1,462
- Reporting signal score
- 2,503.96
- Event
- duodenal ulcer perforation
- Reports
- 615
- Reporting signal score
- 2,515.69
- Event
- fatigue
- Reports
- 2,713
- Reporting signal score
- 2,188.88
- Event
- febrile neutropenia
- Reports
- 384
- Reporting signal score
- 299.14
- Event
- folliculitis
- Reports
- 335
- Reporting signal score
- 956.155
- Event
- gastrointestinal disorder
- Reports
- 379
- Reporting signal score
- 384.384
- Event
- gastrointestinal toxicity
- Reports
- 80
- Reporting signal score
- 190.239
- Event
- general physical health deterioration
- Reports
- 625
- Reporting signal score
- 755.875
- Event
- glossodynia
- Reports
- 2,063
- Reporting signal score
- 8,240.59
- Event
- haematotoxicity
- Reports
- 139
- Reporting signal score
- 211.14
And 53 more, listed on the interactive page.
- NCT00005586
- NCT00081289
- NCT00192075
- NCT00209703
- NCT00268398
- NCT00291785
- NCT00323011
- NCT00524706
- NCT01183780
- NCT01442649
- NCT01442935
- NCT01628211
- NCT01802645
- NCT02141295
- NCT02688023
- NCT03530267
- NCT05018182
- NCT00143403
- NCT00385021
- NCT01289821
- NCT01765582
- NCT02384850
- NCT02842580
- NCT02885753
- NCT02426450
And 70 more, listed on the interactive page.
- Dose
- 1-2 mg/kg/day (for weight less than 40 kg)
- Route
- Oral
- How often
- Once daily or in divided doses up to 6 times per day
- Do not crush tablets
- Take with or without food
- Hydrogen bond acceptors
- 9
- Hydrogen bond donors
- 7
- Polar surface area
- 219.84
- Calculated partition coefficient (ALogP)
- -0.73
- Calculated partition coefficient (XLogP)
- -1.2
- Prodrug
- No
- Chirality
- Racemic
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 10
- Heavy atoms
- 34
- Molecular formula
- C20H23N7O7
- Monoisotopic mass
- 473.16589610
- Natural product
- Yes
- 64661-217
- 64661-650
- Recorded assays
- 701
- Active assays
- 4
- Confirmatory
- Other
- Antidotes
- Vitamin B Complex
Related records
Trials (688)
- 2 Versus 6 Hour Oxaliplatin Infusions in Patients With Gastrointestinal Cancers
- 5-Fluorouracil, Bevacizumab, and Radiation Followed by Modified FOLFOX6 and Bevacizumab in Stage II/III Rectal Cancer
- 5-FU, Folinic Acid and Irinotecan (FOLFIRI) Plus Cetuximab Versus FOLFIRI Plus Bevacizumab in First Line Treatment Colorectal Cancer (CRC)
- 5-FU, Leucovorin, Oxaliplatin and Docetaxel (FLOT) Versus Epirubicin, Cisplatin and 5-FU (ECF) in Patients With Locally Advanced, Resectable Gastric Cancer
- 5FU/LV, Irinotecan, Temozolomide and Bevacizumab for MGMT Silenced, Microsatellite Stable Metastatic Colorectal Cancer.
- A Clinical Study of Calderasib (MK-1084) With Targeted Therapy and Chemotherapy in People With Colorectal Cancer (MK-1084-012/KANDLELIT-012)
- A Clinical Trial of a New Combination Treatment, Domvanalimab and Zimberelimab, Plus Chemotherapy, for People With an Upper Gastrointestinal Tract Cancer That Cannot be Removed With Surgery That Has Spread to Other Parts of the Body
- A Clinical Trial of CoFactor Formulations and Leucovorin Administered Intravenously in Healthy, Adult Subjects.
- A Dose Escalation Study of MM-398 Plus Irinotecan in Patients With Unresectable Advanced Cancer
- A Folinic Acid Intervention for Autism Spectrum Disorders
- A Multi-center Randomized Controlled Trial of Intraportal Chemotherapy Combined With Adjuvant Chemotherapy (mFOLFOX6) for Stage II and III Colon Cancer
- A Multicenter Trial Comparing Induction C/T Followed by CCRT v.s. CCRT Alone in Stage IV Nasopharyngeal Carcinoma
- A Novel "Pediatric-Inspired" Regimen With Reduced Myelosuppressive Drugs for Adults (Aged 18-60) With Newly Diagnosed Ph Negative Acute Lymphoblastic Leukemia
- A Phase 1 Study of Pegilodecakin (LY3500518) in Participants With Advanced Solid Tumors
- A Phase 1/2 Study of INCB001158 in Combination With Chemotherapy in Subjects With Solid Tumors
- A Phase I Study of Aflibercept Plus FOLFIRI (Irinotecan, 5-Fluorouracil, and Leucovorin) in Chinese Patients With Advanced Solid Malignancies
- A Phase I Study of Isolated Hepatic Perfusion With Escalating Dose Melphalan Followed by Postoperative Hepatic Arterial Floxuridine and Leucovorin for Metastatic Unresectable Colorectal Cancers of the Liver
- A Phase I Study of Weekly Gemcitabine in Combination With Infusional Fluorodeoxyuridine and Oral Calcium Leucovorin in Adult Cancer Patients
- A Phase I Trial of 5-Fluorouracil Given With 776C85 (GW776) and Low-Dose Leucovorin in Adult Patients With Solid Tumors
- A Phase I Trial of HDFL48 in Recurrent or Metastatic Colorectal Cancers
In development for (39)
- Adenocarcinoma Phase 2
- Autism Phase 2
- Autism spectrum disorder Phase 2
- Autism spectrum disorder 1 Phase 2
- Biliary tract cancer Phase 2
- Biliary tract disorder Phase 2
- Bone sarcoma Phase 2
- Cancer Phase 2
- Cholangiocarcinoma Phase 2
- Colon carcinoma Phase 2
- Colorectal adenocarcinoma Phase 3
- Colorectal cancer Phase 3
- Colorectal carcinoma Phase 3
- Colorectal neoplasm Phase 3
- Depressive disorder Phase 3
- Down syndrome Phase 3
- Esophageal cancer Phase 2
- Esophageal squamous cell carcinoma Phase 2
- Exocrine pancreatic carcinoma Phase 3
- Gastric adenocarcinoma Phase 3