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10872 details
Primary information
ID10872
Therapeutic IDTh1232
Protein NameLenograstim
SequenceNA
Molecular Weight18668
Chemical FormulaC840-H1330-N222-O242-S8
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeThe 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.
DescriptionLenograstim is a recombinant granulocyte colony-stimulating factor which functions as an immunostimulator.
Indication/DiseaseThe drug is used to reduce the risk of life-threatening infection in patients with neutropenia, particularly after cytotoxic chemotherapy. GRANOCYTE ( 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. GRANOCYTE is also indicated to mobilise peripheral blood progenitor cells (PBPCs) with GRANOCYTE alone, or after myelosuppressive chemotherapy, in order to accelerate haematopoietic recovery by infusion of such cells, after myelosuppressive or myeloablative therapy. GRANOCYTE 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).
PharmacodynamicsLenograstim 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 PBSC mobilisation.
Mechanism of ActionLenograstim 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.
ToxicitySpecies 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
MetabolismLenograstim is metabolised to peptides.
AbsorptionDuring 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.
Apparent distribution volume (Vd area) is approximately 52 ± 5 mL/kg body weight.
ClearancePlasma clearance of lenograstim increased 3-fold (from 50 up to 150 mL/min) during repeated sc dosing.
CategoriesAntineoplastic and Immunomodulating Agents
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetGranulocyte colony-stimulating factor receptor
Brand NameGranocyte
CompanyNA
Brand DescriptionNA
Prescribed ForReducing the duration of neutropenia and risk of infection in people treated with chemotherapy for cancer.
Chemical NameL-treonine-colony-stimulating factor
FormulationNA
Physical Appearance Solid
Route of AdministrationSubcutaneous or Intravenous
Recommended DosageNA
ContraindicationPeople with malignancies affecting myeloid cell
Side EffectsDecrease in the number of platelets in the blood (thrombocytopenia), Headache, Feeling weak, Bone pain, Back pain, Elevated levels of liver enzymes
Useful Link 1Link
Useful Link 2NA
RemarksNA