Levoleucovorin
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Also known as (6s)-leucovorin(s)-leucovorinKhapzoryL-folinic acidLevofoleneLevofolinic acidLFP-754Calcium levofolinate (Calcium Folinate)
Summary
Levoleucovorin (CHEMBL1908841) is an approved small-molecule antineoplastic agent; indicated across 9 conditions including colorectal carcinoma and osteosarcoma.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- Indications: 9 conditions
- Clinical trials: 21
- Chemistry: 473.4 Da · C20H23N7O7
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1908841 |
| Name | Levoleucovorin |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 135398559 |
| ChEBI | CHEBI:63606 |
| Molecular formula | C20H23N7O7 |
| Molecular weight | 473.4 |
| InChIKey | VVIAGPKUTFNRDU-STQMWFEESA-N |
SMILES: C1[C@@H](N(C2=C(N1)N=C(NC2=O)N)C=O)CNC3=CC=C(C=C3)C(=O)N[C@@H](CCC(=O)O)C(=O)O
IUPAC name: (2S)-2-[[4-[[(6S)-2-amino-5-formyl-4-oxo-3,6,7,8-tetrahydropteridin-6-yl]methylamino]benzoyl]amino]pentanedioic acid
ChEBI definition: The pharmacologically active (6S)-stereoisomer of 5-formyltetrahydrofolic acid.
Pharmacological roles (ChEBI): antineoplastic agent.
Other ChEBI roles (chemical / environmental): metabolite.
Also known as: (6s)-leucovorin, (s)-leucovorin, Khapzory, L-folinic acid, Levofolene, Levofolinic acid, Levoleucovorin, LFP-754, LEVOLEUCOVORIN, Calcium levofolinate (Calcium Folinate)
Parent form; salt/anhydrous children: CHEMBL1908361, CHEMBL3707343
Patent coverage: 401 distinct patent families (857 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 529 (62%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
No target linkage available.
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
9 indications (5 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| colorectal carcinoma | 4 | MONDO:0024331 | EFO:1001951 |
| osteosarcoma | 4 | MONDO:0009807 | EFO:0000637 |
| anemia | 4 | MONDO:0002280 | MONDO:0002280 |
| colorectal neoplasm | 4 | MONDO:0005335 | EFO:0004142 |
| esophageal squamous cell carcinoma | 3 | MONDO:0005580 | EFO:0005922 |
| rectal cancer | 2 | MONDO:0006519 | EFO:1000657 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| colonic neoplasm | 1 | MONDO:0005401 | EFO:0004288 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 21.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 10 |
| PHASE2 | 7 |
| PHASE1/PHASE2 | 4 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03007147 | PHASE3 | ACTIVE_NOT_RECRUITING | Imatinib Mesylate and Combination Chemotherapy in Treating Patients With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia |
| NCT04210115 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Pembrolizumab (MK-3475) Versus Placebo in Participants With Esophageal Carcinoma Who Are Receiving Chemotherapy and Radiation Therapy (MK-3475-975/KEYNOTE-975) |
| NCT04949256 | PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety of Pembrolizumab (MK-3475) Plus Lenvatinib (E7080/MK-7902) Plus Chemotherapy in Participants With Metastatic Esophageal Carcinoma (MK-7902-014/E7080-G000-320/LEAP-014) |
| NCT05253651 | PHASE3 | RECRUITING | A Study of Tucatinib With Trastuzumab and mFOLFOX6 Versus Standard of Care Treatment in First-line HER2+ Metastatic Colorectal Cancer |
| NCT06041477 | PHASE3 | RECRUITING | Concurrently vs Sequentially Combined HAIC With Targeted and Immunotherapy in Potentially Resectable HCC |
| NCT06509126 | PHASE3 | RECRUITING | Intermittent or Continuous Panitumumab Plus FOLFIRI for Left Sided RAS/B-RAF Wild-type Metastatic Colorectal Cancer |
| NCT06662786 | PHASE3 | RECRUITING | A Study of Amivantamab and mFOLFOX6 or FOLFIRI Versus Cetuximab and mFOLFOX6 or FOLFIRI as First-line Treatment in Participants With KRAS/NRAS and BRAF Wild-type Unresectable or Metastatic Left-sided Colorectal Cancer |
| NCT06750094 | PHASE3 | RECRUITING | A Study of Amivantamab and FOLFIRI Versus Cetuximab/Bevacizumab and FOLFIRI in Participants With KRAS/NRAS and BRAF Wild-type Colorectal Cancer Who Have Previously Received Chemotherapy |
| NCT01926236 | PHASE3 | COMPLETED | Active Symptom Control Alone or With mFOLFOX Chemotherapy for Locally Advanced/ Metastatic Biliary Tract Cancers |
| NCT04456699 | PHASE3 | COMPLETED | Efficacy and Safety of Olaparib (MK-7339) With or Without Bevacizumab Compared to Bevacizumab With a Fluoropyrimidine in Unresectable or Metastatic Colorectal Cancer (CRC) (MK-7339-003/LYNK-003) |
| NCT05945823 | PHASE2 | ACTIVE_NOT_RECRUITING | Phase 2 Futibatinib in Combination With PD-1 Antibody Based Standard of Care in Solid Tumors |
| NCT06317662 | PHASE2 | RECRUITING | Testing the Addition of the Anti-cancer Drug Venetoclax and/or the Anti-cancer Immunotherapy Blinatumomab to the Usual Chemotherapy Treatment for Infants With Newly Diagnosed KMT2A-rearranged or KMT2A-non-rearranged Leukemia |
| NCT06469944 | PHASE1/PHASE2 | RECRUITING | Substudy 06C: A Study of Investigational Agents With Pembrolizumab (MK-3475) and Chemotherapy in Participants With First-Line Locally Advanced Unresectable/Metastatic Gastroesophageal Adenocarcinoma (MK-3475-06C/KEYMAKER-U06) |
| NCT06780111 | PHASE1/PHASE2 | RECRUITING | Substudy 06E: Umbrella Study of Combination Therapies in Esophageal Cancer (MK-3475-06E/KEYMAKER-U06) |
| NCT01383707 | PHASE2 | COMPLETED | A Study of Bevacizumab and Modified FOLFOX-6 (mFOLFOX-6) in Participants With Metastatic Colorectal Cancer |
| NCT01481545 | PHASE2 | COMPLETED | Bevacizumab With Pelvic Radiotherapy And Primary Chemotherapy in Patients With Poor-Risk Rectal Cancer |
| NCT01590719 | PHASE2 | COMPLETED | A Study of Onartuzumab (MetMAb) in Combination With mFOLFOX6 in Patients With Metastatic Human Epidermal Growth Factor Receptor 2 (HER2) Negative Gastroesophageal Cancer |
| NCT01681472 | PHASE1/PHASE2 | COMPLETED | PK/PD Investigation of Modufolin (Arfolitixorin) in Plasma, Tumor and Adjacent Mucosa Adjacent Mucosa in Patients With Colon Cancer |
| NCT03222089 | PHASE2 | WITHDRAWN | Phase II Trial of FOLFOXIGIL Versus FOLFOXIRI as First-line Therapy in Patients With mCRC |
| NCT03294252 | PHASE1/PHASE2 | TERMINATED | Oxaliplatin in PIPAC for Nonresectable Peritoneal Metastases of Digestive Cancers |
| NCT03698461 | PHASE2 | COMPLETED | Treatment of Colorectal Liver Metastases With Immunotherapy and Bevacizumab |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).