Lenograstim

Identification

Summary

Lenograstim is a granulocyte colony-stimulating factor indicated in the reduction of duration of neutropenia in bone marrow transplant and cytotoxic chemotherapy, as well as mobilizing hematopoietic stem cells in healthy donors.

Generic Name
Lenograstim
DrugBank Accession Number
DB13144
Background

Lenograstim is a recombinant granulocyte colony-stimulating factor used as an immunostimulating agent.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Haematopoietic growth factors
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • G-CSF (CHO cell derived)
  • Glycosylated recombinant G-CSF
  • Glycosylated recombinant granulocyte colony stimulating factor
  • Granulocyte colony stimulating factor 3 (CHO cell derived)
  • Granulocyte colony-stimulating factor lenograstim
  • Lenograstim
  • Lenograstim (genetical recombination)
  • Lenograstim rDNA

Pharmacology

Indication

The drug is used to reduce the risk of life-threatening infection in patients with neutropenia, particularly after cytotoxic chemotherapy. Lenograstim is indicated as a treatment to reduce the duration of neutropenia and the severity of infections in patients with non-myeloid malignancy who have undergone autologous or allogeneic bone marrow transplantation, or treatment with established cytotoxic chemotherapy and in addition to reduce the incidence of infection associated with established cytotoxic chemotherapy. Lenograstim is also indicated to mobilise peripheral blood progenitor cells (PBPCs) with Lenograstim alone, or after myelosuppressive chemotherapy, in order to accelerate haematopoietic recovery by infusion of such cells, after myelosuppressive or myeloablative therapy. Lenograstim is also indicated to accelerate the engraftment of these cells after their reinfusion.

GRANOCYTE is also indicated for the treatment of severe chronic neutropenia including congenital agranulocytosis (Kostmann's syndrome).

Pharmacology
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Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Lenograstim has been confirmed as a valuable adjunct to minimise the haematological toxicity of myelosuppressive chemotherapy in patients with malignant disease. The drug also enhances neutrophil recovery in patients undergoing stem cell rescue, and assists peripheral blood progenitor cells mobilisation.

Mechanism of action

Lenograstim is the glycosylated recombinant form of human granulocyte colony stimulating factor. Lenograstim accelerates neutrophil recovery significantly after chemotherapy, with beneficial effects on clinical end-points such as incidence of laboratory-confirmed infection and length of hospital stay. Chemotherapy dose intensity has also been increased in patients receiving lenograstim, notably those with breast or small cell lung cancer, although improvements in tumour response and survival have not been demonstrated. Lenograstim also assists neutrophil recovery in patients undergoing bone marrow transplantation, and stimulates the production of peripheral blood stem cells (PBSCs) for autologous transfusion after aggressive chemotherapy.

TargetActionsOrganism
AGranulocyte colony-stimulating factor receptor
agonist
Humans
Absorption

During repeated dosing (iv and sc routes), peak serum concentrations (at the end of iv infusion or after sc injection) are proportional to the injected dose. Repeated dosing with lenograstim by the two injection routes results in no evidence of drug accumulation.

Volume of distribution

Apparent distribution volume (Vd area) is approximately 52 ± 5 mL/kg body weight.

Protein binding

Not Available

Metabolism

Lenograstim is metabolised to peptides.

Route of elimination

Lenograstim is poorly excreted in urine as intact compound (less than 1% of the dose).

Half-life

The pharmacokinetic profile of lenograstim is similar in healthy volunteers and cancer patients with elimination half-life (t½β) values of 2.3 - 3.3 hrs (volunteers); 2.8-7.5 hrs (cancer patients) following sc administration, and 0.8 - 2.1 hrs (volunteers); 1.1 - 4.0 hrs (cancer patients) following iv administration.

Clearance

Plasma clearance of lenograstim increased 3-fold (from 50 up to 150 mL/min) during repeated sc dosing.

Adverse Effects
Adverseeffects
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Toxicity

Species observed : Human (Man) Test type: TDLo ( Lowest Published Toxic Dose) Route of exposure: Subcutaneous Dose/Duration: 21428mg/kg/15 Toxic Effect: Skin and appendages: Dermatitis, allergic ( after systemic exposure )

Species observed : Rodent - Rat Test type: LD50 Route of exposure: Oral Dose/Duration: >5mg/kg Toxic Effect: Details of toxic effects not reported other than lethal dose value

Species observed : Rodent - Rat Test type: LD50 Route of exposure: Subcutaneous Dose/Duration: >5mg/kg Toxic Effect: Details of toxic effects not reported other than lethal dose value

Species observed : Rodent - Rat Test type: LD50 Route of exposure: Intravenous Dose/Duration: >5mg/kg Toxic Effect: Details of toxic effects not reported other than lethal dose value

Species observed : Mammal - Dog Test type: LD50 Route of exposure: Intravenous Dose/Duration: >5mg/kg Toxic Effect: Details of toxic effects not reported other than lethal dose value

Species observed : Mammal - Dog Test type: LD50 Route of exposure: Subcutaneous Dose/Duration: >5mg/kg Toxic Effect: Details of toxic effects not reported other than lethal dose value

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
CyclophosphamideThe risk or severity of pulmonary toxicity can be increased when Lenograstim is combined with Cyclophosphamide.
TopotecanThe risk or severity of neutropenia can be increased when Lenograstim is combined with Topotecan.
VinblastineThe risk or severity of peripheral neuropathy can be increased when Lenograstim is combined with Vinblastine.
VincristineThe risk or severity of peripheral neuropathy can be increased when Lenograstim is combined with Vincristine.
VindesineThe risk or severity of peripheral neuropathy can be increased when Lenograstim is combined with Vindesine.
VinflunineThe risk or severity of peripheral neuropathy can be increased when Lenograstim is combined with Vinflunine.
VinorelbineThe risk or severity of peripheral neuropathy can be increased when Lenograstim is combined with Vinorelbine.
Interactions
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Food Interactions
Not Available

Products

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International/Other Brands
Granocyte / Neutrogin

Categories

ATC Codes
L03AA10 — Lenograstim
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
6WS4C399GB
CAS number
135968-09-1

References

General References
  1. Dunn CJ, Goa KL: Lenograstim: an update of its pharmacological properties and use in chemotherapy-induced neutropenia and related clinical settings. Drugs. 2000 Mar;59(3):681-717. [Article]
  2. Medsafe [Link]
  3. ChemIDPlus [Link]
  4. AIFA Product Information: Myelostim (lenograstim) powder for injection [Link]
PubChem Substance
347911430
RxNav
70167
Wikipedia
Lenograstim

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentMyocardial Infarction1
4CompletedTreatmentNeoplasms (no Otherwise Specified)1
3CompletedTreatmentAcute Myeloid Leukemia (AML)1
3CompletedTreatmentBreast Cancer3
3RecruitingTreatmentRefractory, metastatic hormone-refractory Prostate cancer1
3Unknown StatusPreventionG-CSF, Multiple Myeloma, Febrile Episode, Filgrastim, Leograstim1
3Unknown StatusTreatmentDiffuse Large B-Cell Lymphoma (DLBCL) / IPI≥21
2CompletedTreatmentAcute Myeloid Leukemia (AML)1
2CompletedTreatmentDilated Cardiomyopathy (DCM)1
2RecruitingTreatmentProstate Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, for solutionIntravenous; Subcutaneous13000.000 IU/ml
Injection, powder, for solutionIntravenous; Subcutaneous263 mcg
Injection, powder, for solutionIntravenous; Subcutaneous
Injection, powder, lyophilized, for solutionIntravenous
Injection, powder, for solutionIntravenous; Subcutaneous13 million IU/ml
Injection, powder, for solutionIntravenous; Subcutaneous34 million IU/ml
Powder100 mcg/1vial
Powder250 mcg/1vial
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Receptor activity
Specific Function
Receptor for granulocyte colony-stimulating factor (CSF3), essential for granulocytic maturation. Plays a crucial role in the proliferation, differientation and survival of cells along the neutroph...
Gene Name
CSF3R
Uniprot ID
Q99062
Uniprot Name
Granulocyte colony-stimulating factor receptor
Molecular Weight
92155.615 Da
References
  1. UniProt [Link]
  2. KEGG [Link]

Drug created on November 15, 2016 20:43 / Updated on June 08, 2021 11:32