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eflornithine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 990 | 70052-12-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Eflornithine is an irreversible inhibitor of the enzyme ornithine decarboxylase (ODC), the first and rate-limiting enzyme in the biosynthesis of polyamines and a transcriptional target of MYCN. Polyamines are involved in differentiation and proliferation of mammalian cells and are important for neoplastic transformation. Inhibition of polyamine synthesis by eflornithine restored the balance of the LIN28/Let-7 metabolic pathway, which is involved in regulation of cancer stem cells and glycolytic metabolism, by decreasing expression of the oncogenic drivers MYCN and LIN28B in MYCN-amplified neuroblastoma. In vitro, eflornithine induced senescence and suppressed neurosphere formation in MYCN-amplified and MYCN non-amplified neuroblastoma cells, indicating a cytostatic effect. Treatment with eflornithine prevented or delayed tumor formation in mice injected with limiting dilutions of MYCN-amplified neuroblastoma cells.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 55 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,EIF2AK3,ERBB2,GRK2,ITK,JAK3,MAP2K6,MAPK10,MAPK7,NTRK1,NTRK2,PDK2,PDK4,PRKDC,SYK,TEK,TGFBR1,ZAP70 | 24 | |||
| kinase-selectivity-class | AXL,EIF2AK3,MAP2K6 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 28, 1990 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | D11AX16 | DERMATOLOGICALS OTHER DERMATOLOGICAL PREPARATIONS OTHER DERMATOLOGICAL PREPARATIONS Other dermatologicals |
| ATC | L01XX79 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| ATC | P01CX03 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS Other agents against leishmaniasis and trypanosomiasis |
| FDA EPC | N0000175485 | Antiprotozoal |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D000981 | Antiprotozoal Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D014344 | Trypanocidal Agents |
| MeSH PA | D065108 | Ornithine Decarboxylase Inhibitors |
| FDA MoA | N0000175844 | Decarboxylase Inhibitors |
| FDA EPC | N0000175845 | Decarboxylase Inhibitor |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:36335 | trypanocidal drug |
| CHEBI has role | CHEBI:70868 | antileishmanial agent |
Related Drugs by ATC class:
D11AX Other dermatologicals 20 drugs
L01XX Other antineoplastic agents 33 drugs
P01CX Other agents against leishmaniasis and trypanosomiasis 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| African trypanosomiasis | indication | 27031003 | DOID:10112 |
| Female Facial Hirsutism | indication | ||
| Reduce the risk of relapse for high-risk neuroblastoma (HRNB) | indication | ||
| Eruption of skin | contraindication | 271807003 | DOID:0050486 |
| Skin irritation | contraindication | 367466007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 1.31 | acidic |
| pKa2 | 10.94 | Basic |
| pKa3 | 5.21 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 192MG BASE | IWILFIN | USWM | N215500 | Dec. 13, 2023 | RX | TABLET | ORAL | 12582625 | Feb. 12, 2036 | TREATMENT TO REDUCE THE RISK OF RELAPSE IN ADULT AND PEDIATRIC PATIENTS WITH HIGH-RISK NEUROBLASTOMA (HRNB) WHO HAVE DEMONSTRATED AT LEAST A PARTIAL RESPONSE TO PRIOR MULTIAGENT, MULTIMODALITY THERAPY INCLUDING ANTI-GD2 IMMUNOTHERAPY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 192MG BASE | IWILFIN | USWM | N215500 | Dec. 13, 2023 | RX | TABLET | ORAL | Dec. 13, 2026 | NEW PRODUCT |
| EQ 192MG BASE | IWILFIN | USWM | N215500 | Dec. 13, 2023 | RX | TABLET | ORAL | Dec. 13, 2030 | TO REDUCE THE RISK OF RELAPSE IN ADULT AND PEDIATRIC PATIENTS WITH HIGH-RISK NEUROBLASTOMA (HRNB) WHO HAVE DEMONSTRATED AT LEAST A PARTIAL RESPONSE TO PRIOR MULTIAGENT, MULTIMODALITY THERAPY INCLUDING ANTI-GD2 IMMUNOTHERAPY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Ornithine decarboxylase | Enzyme | INHIBITOR | Kd | 4.89 | IUPHAR | CHEMBL | |||
| Ornithine decarboxylase | Enzyme | INHIBITOR | DRUG LABEL | SCIENTIFIC LITERATURE | |||||
| Ornithine decarboxylase | Enzyme | Ki | 4.41 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D00829 | KEGG_DRUG |
| 68278-23-9 | SECONDARY_CAS_RN |
| 96020-91-6 | SECONDARY_CAS_RN |
| 4020660 | VANDF |
| 4023581 | VANDF |
| C0002260 | UMLSCUI |
| CHEBI:41948 | CHEBI |
| CHEMBL830 | ChEMBL_ID |
| DB06243 | DRUGBANK_ID |
| CHEMBL1201037 | ChEMBL_ID |
| D000518 | MESH_DESCRIPTOR_UI |
| 3009 | PUBCHEM_CID |
| 5551 | INN_ID |
| 5176 | IUPHAR_LIGAND_ID |
| ZQN1G5V6SR | UNII |
| 284913 | RXNORM |
| 15655 | MMSL |
| 35968 | MMSL |
| 37870 | MMSL |
| d10151 | MMSL |
| 005117 | NDDF |
| 005118 | NDDF |
| 019746 | NDDF |
| 108715006 | SNOMEDCT_US |
| 108716007 | SNOMEDCT_US |
| 1269007006 | SNOMEDCT_US |
| 372533004 | SNOMEDCT_US |
| 783271002 | SNOMEDCT_US |
| DMO | PDB_CHEM_ID |
| ZQN1G5V6SR | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| VANIQA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5124 | CREAM | 139 mg | TOPICAL | NDA | 19 sections |
| iwilfin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 78670-150 | TABLET | 250 mg | ORAL | NDA | 27 sections |
| Florexa | HUMAN PRESCRIPTION DRUG LABEL | 1 | 82160-125 | CREAM | 4170 mg | TOPICAL | unapproved drug other | 16 sections |