AI ASSISTANT
Ask DrugCentral
Explore drug information in your own words.
Type a question in the search bar above to get started. Each question is answered independently.
AI can make mistakes. Verify answers against the original sources before relying on them.
lefamulin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibacterials, pleuromulin derivatives | 5348 | 1061337-51-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
XENLETA is a semi-synthetic antibacterial agent for oral and intravenous administration. Lefamulin inhibits bacterial protein synthesis through interactions (hydrogen bonds, hydrophobic interactions, and Van der Waals forces) with the A- and P-sites of the peptidyl transferase center (PTC) in domain V of the 23s rRNA of the 50S subunit. The binding pocket of the bacterial ribosome closes around the mutilin core for an induced fit that prevents correct positioning of tRNA.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 1.32 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3.96 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.17 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 6.40 hours | Lombardo F, Berellini G, Obach RS |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 21 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK3,MAP2K6,MAP3K7,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,STK33,SYK,TEK,TGFBR1,ZAP70 | 32 | |||
| kinase-selectivity-class | EIF2AK3 | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 19, 2019 | FDA | NABRIVA |
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 | J01XX12 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER ANTIBACTERIALS Other antibacterials |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| FDA CS | M0006609 | Diterpenes |
| FDA EPC | N0000175434 | Pleuromutilin Antibacterial |
| FDA MoA | N0000182141 | Cytochrome P450 3A4 Inhibitors |
| FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
| CHEBI has role | CHEBI:33281 | antimicrobial agent |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
Related Drugs by ATC class:
J01XX Other antibacterials 12 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pneumonia due to Streptococcus | indication | 34020007 | |
| Pneumonia due to Mycoplasma pneumoniae | indication | 46970008 | |
| Bacterial pneumonia | indication | 53084003 | DOID:874 |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Legionella pneumonia | indication | 195889001 | |
| Pneumonia due to Staphylococcus aureus | indication | 441658007 | |
| Pneumonia caused by Chlamydia pneumoniae | indication | 724498004 | |
| Bronchopneumonia due to Haemophilus influenzae | indication | 10625231000119106 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.21 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 600MG BASE | XENLETA | HONG KONG | N211672 | Aug. 19, 2019 | RX | TABLET | ORAL | Aug. 19, 2024 | NEW CHEMICAL ENTITY |
| EQ 150MG BASE/15ML (EQ 10MG BASE/ML) | XENLETA | HONG KONG | N211673 | Aug. 19, 2019 | RX | SOLUTION | INTRAVENOUS | Aug. 19, 2024 | NEW CHEMICAL ENTITY |
| EQ 600MG BASE | XENLETA | HONG KONG | N211672 | Aug. 19, 2019 | RX | TABLET | ORAL | Aug. 19, 2029 | GENERATING ANTIBIOTIC INCENTIVES NOW |
| EQ 150MG BASE/15ML (EQ 10MG BASE/ML) | XENLETA | HONG KONG | N211673 | Aug. 19, 2019 | RX | SOLUTION | INTRAVENOUS | Aug. 19, 2029 | GENERATING ANTIBIOTIC INCENTIVES NOW |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Multidrug resistance protein 1 | Transporter | IC50 | 4.47 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 21904A5386 | UNII |
| 1350636-82-6 | SECONDARY_CAS_RN |
| 4038663 | VANDF |
| C4482908 | UMLSCUI |
| CHEBI:755252 | CHEBI |
| 62B | PDB_CHEM_ID |
| CHEMBL3291398 | ChEMBL_ID |
| 58076382 | PUBCHEM_CID |
| DB12825 | DRUGBANK_ID |
| CHEMBL3545309 | ChEMBL_ID |
| D11631 | KEGG_DRUG |
| 9849 | INN_ID |
| C000591018 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10824 | IUPHAR_LIGAND_ID |
| 789396009 | SNOMEDCT_US |
| 789501006 | SNOMEDCT_US |
| 321702 | MMSL |
| 37323 | MMSL |
| d09356 | MMSL |
| 018094 | NDDF |
| 018095 | NDDF |
| 2198943 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Xenleta | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71288-037 | TABLET, COATED | 600 mg | ORAL | NDA | 27 sections |
| Xenleta | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71288-039 | INJECTION, SOLUTION | 150 mg | INTRAVENOUS | NDA | 27 sections |
| Xenleta | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72000-110 | TABLET, COATED | 600 mg | ORAL | NDA | 27 sections |
| Xenleta | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72000-120 | INJECTION, SOLUTION | 150 mg | INTRAVENOUS | NDA | 27 sections |