Overview
Lipegfilgrastim, previously known as XM22, is a pegylated, recombinant granulocyte colony-stimulating factor (G-CSF) that was synthetized using a highly site-specific glycoPEGylation technology . It is used as an alternate to Pegfilgrastim for prophylactic use in cancer patients receiving chemotherapy and at risk for developing chemotherapy-induced neutropenia. Since July 2013, lipegfilgrastim is marketed by the EMA as Lonquex for subcutaneously injection, where it is administered once following cytotoxic chemotherapy for each chemotherapy cycle in adult patients being treated with cytotoxic chemotherapy for malignancy. It aims to reduce the duration of neutropenia and the incidence of febrile neutropenia. Neutropenia and febrile neutropenia (FN) are frequent and potentially fatal complications that occur from myelosuppressive anticancer treatments . Severe chemotherapy-induced neutropenia and febrile neutropenia significantly increases the risk for life-threatening infection and sepsis. Granulocyte colony-stimulating factors (G-CSFs) were introduced in the 1980's to the clinical setting to stimulate neutrophil proliferation and differentiation, thereby reducing the duration and severity of chemotherapy-induced neutropenia . Lipegfilgrastim is a covalent conjugate of Filgrastim with a single methoxy polyethylene glycol (PEG) molecule via a carbohydrate linker consisting of glycine, N-acetylneuraminic acid and N-acetylgalactosamine . The average molecular mass of lipegfilgrastim comprises 18,798 Da for Filgrastim, 203 Da for GalNAc, 338 Da for glycylsialic acid and approximately 20,000 Da for PEG . PEG moiety protects the active molecule from enzyme degradation, which allows longer half-life of drug and less frequent dosing-schedule in addition to acceptable safety and efficacy profile .
Indication
Indicated for the reduction in the duration of neutropenia and the incidence of febrile neutropenia in adult patients treated with cytotoxic chemotherapy for malignancy (with the exception of chronic myeloid leukaemia and myelodysplastic syndromes) .
Associated Conditions
- Febrile Neutropenia
- Neutropenia
Research Report
Lipegfilgrastim (Lonquex®): A Comprehensive Monograph on a Novel GlycoPEGylated Granulocyte Colony-Stimulating Factor
Executive Summary
Lipegfilgrastim, marketed under the brand name Lonquex®, is a long-acting recombinant human granulocyte colony-stimulating factor (G-CSF) developed for supportive care in oncology. Its primary indication is the reduction of the duration of neutropenia and the incidence of its life-threatening complication, febrile neutropenia, in cancer patients undergoing myelosuppressive chemotherapy. Lipegfilgrastim represents a significant advancement in the G-CSF class, distinguished by its unique molecular structure derived from a highly site-specific glycoPEGylation technology. This process covalently attaches a single polyethylene glycol (PEG) moiety to the filgrastim protein backbone via a carbohydrate linker at a precise location, resulting in a more homogenous molecular entity compared to conventionally pegylated G-CSFs.
Pharmacologically, lipegfilgrastim functions as an agonist at the G-CSF receptor, mimicking the endogenous protein to stimulate the proliferation, differentiation, and release of neutrophils from the bone marrow. The PEG moiety extends its plasma half-life, enabling a convenient once-per-chemotherapy-cycle dosing regimen. Its clearance is governed by a self-regulating, neutrophil-mediated mechanism, which maintains higher drug concentrations during periods of severe neutropenia and accelerates clearance as neutrophil counts recover.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2015/08/19 | N/A | Completed | Beaumont Hospital | ||
2014/12/03 | Phase 1 | Completed | |||
2014/01/23 | Phase 3 | Completed | |||
2012/04/26 | Phase 1 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
No FDA approvals found for this drug. |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
---|---|---|---|
Authorised | 7/25/2013 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
LONQUEX SOLUTION FOR INJECTION IN PRE-FILLED SYRINGE 6MG/0.6ML | SIN16019P | INJECTION, SOLUTION | 6.00 mg/0.6ml | 9/25/2020 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
---|---|---|---|---|---|
No NMPA approvals found for this drug. |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
---|---|---|---|---|---|
No PPB approvals found for this drug. |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
---|---|---|---|---|---|
LONQUEX lipegfilgrastim (rbe) 6 mg/0.6 mL solution for injection prefilled syringe | 231016 | Medicine | A | 11/12/2015 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
---|---|---|---|---|---|
No Health Canada approvals found for this drug. |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
---|---|---|---|---|---|
Lonquex 6mg solucion inyectable | 113856001 | SOLUCIÓN INYECTABLE | Uso Hospitalario | Not Commercialized | |
LONQUEX 6 MG/0,6 ML SOLUCION INYECTABLE | 1130856004 | SOLUCIÓN INYECTABLE | Uso Hospitalario | Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Philippines FDA approvals found for this drug. |
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Saudi SFDA approvals found for this drug. |
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
No Malaysia NPRA approvals found for this drug. |
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
---|---|---|---|---|---|
No UK EMC drug information found for this drug. |
Help Us Improve
Your feedback helps us provide better drug information and insights.