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| Primary information |
|---|
| ID | 10872 |
| Therapeutic ID | Th1232 |
| Protein Name | Lenograstim |
| Sequence | NA
|
| Molecular Weight | 18668 |
| Chemical Formula | C840-H1330-N222-O242-S8 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| 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. |
| Description | Lenograstim is a recombinant granulocyte colony-stimulating factor which functions as an immunostimulator. |
| Indication/Disease | The 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). |
| 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 PBSC 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. |
| 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 |
| Metabolism | Lenograstim is metabolised to peptides. |
| 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. |
| Apparent distribution volume (Vd area) is approximately 52 ± 5 mL/kg body weight. |
| Clearance | Plasma clearance of lenograstim increased 3-fold (from 50 up to 150 mL/min) during repeated sc dosing. |
| Categories | Antineoplastic and Immunomodulating Agents |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Granulocyte colony-stimulating factor receptor |
| Brand Name | Granocyte |
| Company | NA |
| Brand Description | NA |
| Prescribed For | Reducing the duration of neutropenia and risk of infection in people treated with chemotherapy for cancer. |
| Chemical Name | L-treonine-colony-stimulating factor |
| Formulation | NA |
| Physical Appearance | Solid |
| Route of Administration | Subcutaneous or Intravenous |
| Recommended Dosage | NA |
| Contraindication | People with malignancies affecting myeloid cell |
| Side Effects | Decrease in the number of platelets in the blood (thrombocytopenia), Headache, Feeling weak, Bone pain, Back pain, Elevated levels of liver enzymes |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |