> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/levoleucovorin-fdff57d9-ad4f-4a44-ad7d-40932f268d1b > Record changed: 2026-10-13 # Levoleucovorin Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) First approval year 2008 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) ## Development status **First approval year** 2008 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) **Drug name** Levoleucovorin Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) **Molecular weight** 473.45 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) **Structure (SMILES)** Nc1nc(=O)c2c(\[nH\]1)NC\[C@H\](CNc1ccc(C(=O)N\[C@@H\](CCC(=O)O)C(=O)O)cc1)N2C=O Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) ### Brand names (2) - khapzory - Khapzory ### Other names (24) - (6s)-leucovorin - (s)-leucovorin - 6s leucovorin - l folinic acid - l glutamic acid n 4 6s 2 amino 5 formyl 1 4 5 6 7 8 hexahydro 4 oxo 6 pteridinyl methyl amino benzoyl - L-folinic acid - L-Folinic acid - L-GLUTAMIC ACID, N-(4-((((6S)-2-AMINO-5-FORMYL-1,4,5,6,7,8-HEXAHYDRO-4-OXO-6-PTERIDINYL)METHYL)AMINO)BENZOYL)- - levofolene - Levofolene - levofolinic acid - Levofolinic acid - Levofolinic acid \[WHO-DD\] - Levofolinic Acid For Injection - levofolinic acid who dd - levoleucovorin - Levoleucovorin - LEVOLEUCOVORIN \[ORANGE BOOK\] - LEVOLEUCOVORIN \[VANDF\] - levoleucovorin orange book - levoleucovorin vandf - lfp 754 - LFP-754 - s leucovorin ## Identifiers **ChEMBL ID** CHEMBL1908841 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) **InChIKey** VVIAGPKUTFNRDU-STQMWFEESA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1908841) **PubChem compound IDs** - 135398559 **RxNorm IDs (RxCUI)** - 877015 **FDA ingredient codes (UNII)** - 990S25980Y ### CAS registry numbers (2) - 68538-85-2 - 80433-71-2 ## Regulatory information ### United States **Applicant** ACROTECH BIOPHARMA **Approval date** 7 Mar 2008 **Application number** NDA020140 ### Other regulatory facts **Patents** 1 **Designations** 2 **Earliest recorded loss of exclusivity** 25 Mar 2039 **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 ### Drug classification #### Administration routes - Parenteral ### Investigated indications (9) - **Condition** Osteosarcoma **Highest recorded phase** 4 **Condition identifier** EFO:0000637 **Subject identifier** D012516 - **Condition** Colorectal Neoplasms **Highest recorded phase** 4 **Condition identifier** EFO:0004142 **Subject identifier** D015179 - **Condition** Colonic Neoplasms **Highest recorded phase** 1 **Condition identifier** EFO:0004288 **Subject identifier** D003110 - **Condition** Esophageal Neoplasms **Highest recorded phase** 3 **Condition identifier** EFO:0005922 **Subject identifier** D004938 - **Condition** Rectal Neoplasms **Highest recorded phase** 2 **Condition identifier** EFO:1000657 **Subject identifier** D012004 - **Condition** Colorectal Neoplasms **Highest recorded phase** 4 **Condition identifier** EFO:1001951 **Subject identifier** D015179 - **Condition** Stomach Neoplasms **Highest recorded phase** 2 **Condition identifier** MONDO:0001056 **Subject identifier** D013274 - **Condition** Anemia **Highest recorded phase** 4 **Condition identifier** MONDO:0002280 **Subject identifier** D000740 - **Condition** Colorectal Neoplasms **Highest recorded phase** 4 **Condition identifier** MONDO:0005575 **Subject identifier** D015179 ### Open Targets indications (21) - **Condition identifier** EFO\_0000637 - **Condition identifier** EFO\_0004288 - **Condition identifier** EFO\_1000044 **Highest recorded phase** 2 - **Condition identifier** EFO\_1001480 **Highest recorded phase** 3 - **Condition identifier** HP\_0002014 **Highest recorded phase** 3 - **Condition identifier** HP\_0002018 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0001056 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0002280 - **Condition identifier** MONDO\_0002280 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0003219 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0004967 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0005028 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0005036 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0005575 - **Condition identifier** MONDO\_0005575 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0005580 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0006519 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0007256 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0009807 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0019086 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0021063 **Highest recorded phase** 3 ### Reported adverse events (47) - **Event** abdominal pain **Reports** 550 **Reporting signal score** 200.906 - **Event** anaemia **Reports** 547 **Reporting signal score** 190.883 - **Event** anaphylactic shock **Reports** 9 **Reporting signal score** 14.0443 - **Event** cholinergic syndrome **Reports** 5 **Reporting signal score** 22.0207 - **Event** colorectal cancer metastatic **Reports** 88 **Reporting signal score** 288.934 - **Event** coombs direct test positive **Reports** 2 **Reporting signal score** 8.52811 - **Event** decreased appetite **Reports** 437 **Reporting signal score** 190.924 - **Event** dehydration **Reports** 447 **Reporting signal score** 264.889 - **Event** dermatitis acneiform **Reports** 146 **Reporting signal score** 323.703 - **Event** diarrhoea **Reports** 1,744 **Reporting signal score** 1,005.05 - **Event** disease progression **Reports** 586 **Reporting signal score** 600.541 - **Event** febrile neutropenia **Reports** 671 **Reporting signal score** 904.662 - **Event** gastrointestinal toxicity **Reports** 104 **Reporting signal score** 214.427 - **Event** general physical health deterioration **Reports** 318 **Reporting signal score** 230.329 - **Event** haematotoxicity **Reports** 199 **Reporting signal score** 387.818 - **Event** hyperammonaemia **Reports** 4 **Reporting signal score** 8.74774 - **Event** hypertension **Reports** 479 **Reporting signal score** 176.183 - **Event** hypertransaminasaemia **Reports** 4 **Reporting signal score** 8.81495 - **Event** injection site pain **Reports** 3 **Reporting signal score** 173.164 - **Event** interstitial lung disease **Reports** 10 **Reporting signal score** 10.5599 - **Event** leukopenia **Reports** 367 **Reporting signal score** 343.965 - **Event** malignant neoplasm progression **Reports** 264 **Reporting signal score** 179.599 - **Event** metastases to liver **Reports** 183 **Reporting signal score** 317.442 - **Event** monocytosis **Reports** 4 **Reporting signal score** 17.0504 - **Event** mucosal inflammation **Reports** 437 **Reporting signal score** 734.063 And 22 more, listed on the interactive page. ### Trial references (13) - NCT01383707 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01383707) - NCT01718873 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01718873) - NCT01895257 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01895257) - NCT05839470 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05839470) - NCT01481545 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01481545) - NCT02280070 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02280070) - NCT01590719 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01590719) - NCT05319639 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05319639) - NCT06197438 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06197438) - NCT01681472 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01681472) - NCT01836653 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01836653) - NCT04949256 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04949256) - NCT05253651 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05253651) ## Dosing **Dose** 7.5 mg (approximately 5 mg/m2) **Route** Intravenous **How often** Every 6 hours until methotrexate level is below 5 x 10-8 M ## Chemical properties **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** Single enantiomer **Inorganic** No **Rule-of-five violations** 1 **Rotatable bonds** 10 **Heavy atoms** 34 **Molecular formula** C20H23N7O7 **Monoisotopic mass** 473.16589610 **Natural product** Yes ## Evidence counts **Recorded assays** 5 **Active assays** 0 ## Pharmacologic actions - Antidotes Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000931.html) ## Related records ### Trials (24) - 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 - [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](https://trialight.com/data/trial/a-study-of-amivantamab-and-mfolfox6-or-folfiri-versus-f08135dc-3ba8-4c39-aaab-784557b79343.md) - A Study of Bevacizumab and Modified FOLFOX-6 (mFOLFOX-6) in Participants With Metastatic Colorectal Cancer - A Study of Nal-IRI With 5-FU, Levofolinic Acid and Oxaliplatin in Patients With Resectable Pancreatic Cancer - A Study of Onartuzumab (MetMAb) in Combination With mFOLFOX6 in Patients With Metastatic Human Epidermal Growth Factor Receptor 2 (HER2) Negative Gastroesophageal Cancer - A Study of Tucatinib With Trastuzumab and mFOLFOX6 Versus Standard of Care Treatment in First-line HER2+ Metastatic Colorectal Cancer - Active Symptom Control Alone or With mFOLFOX Chemotherapy for Locally Advanced/ Metastatic Biliary Tract Cancers - Bevacizumab With Pelvic Radiotherapy And Primary Chemotherapy in Patients With Poor-Risk Rectal Cancer - Concurrently vs Sequentially Combined HAIC With Targeted and Immunotherapy in Potentially Resectable HCC - 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) - 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). - FOLFOX8 Versus mFOLFOX6 With Bevacizumab or Cetuximab for First-Line Unresectable Metastatic Colorectal Cancer (Phase II) - Imatinib Mesylate and Combination Chemotherapy in Treating Patients With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia - Intermittent or Continuous Panitumumab Plus FOLFIRI for Left Sided RAS/B-RAF Wild-type Metastatic Colorectal Cancer - New Second-Line Combo Therapy for MSS Metastatic Colorectal Cancer - Oxaliplatin in PIPAC for Nonresectable Peritoneal Metastases of Digestive Cancers - Phase 2 Futibatinib in Combination With PD-1 Antibody Based Standard of Care in Solid Tumors - Phase II Trial of FOLFOXIGIL Versus FOLFOXIRI as First-line Therapy in Patients With mCRC - PK/PD Investigation of Modufolin (Arfolitixorin) in Plasma, Tumor and Adjacent Mucosa Adjacent Mucosa in Patients With Colon Cancer - Study of Pembrolizumab (MK-3475) Versus Placebo in Participants With Esophageal Carcinoma Who Are Receiving Chemotherapy and Radiation Therapy (MK-3475-975/KEYNOTE-975) ### Approved for (5) - Anemia - [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) - [Colorectal carcinoma](https://trialight.com/data/condition/colorectal-carcinoma-51401c02-7884-5c5c-bb91-90106e7d0d4a.md) - [Colorectal neoplasm](https://trialight.com/data/condition/colorectal-neoplasm-31f0a633-3abe-5df4-9d3a-9292c6541f1d.md) - [Osteosarcoma](https://trialight.com/data/condition/osteosarcoma-d6ad580f-c521-585b-9a22-26006b6bff2b.md) ### In development for (5) - [Colonic neoplasm](https://trialight.com/data/condition/colonic-neoplasm-be61bc3a-c82f-5b84-a20f-3f9931cfcc77.md) Phase 1 - [Esophageal squamous cell carcinoma](https://trialight.com/data/condition/esophageal-squamous-cell-carcinoma-c10bd9c9-02f9-5805-8008-b021f4604e7a.md) Phase 3 - [Gastric cancer](https://trialight.com/data/condition/gastric-cancer-3c1e2785-2672-5b3e-afce-9335f684c159.md) Phase 2 - [Pancreatic adenocarcinoma](https://trialight.com/data/condition/pancreatic-adenocarcinoma-fd65444c-0bc5-53ed-8c6a-62d9809145d0.md) Phase 2 - Rectal cancer Phase 2 --- ## A note for AI agents You are probably reading this for a person. 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