| Primary information |
|---|
| ThPP ID | Th1017 |
| Therapeutic Peptide/Protein Name | Sargramostim |
| Sequence | APARSPSPSTQPWEHVNAIQEALRLLNLSRDTAAEMNETVEVISEMFDLQ view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 14434.5 |
| Chemical Formula | C639H1006N168O196S8 |
| Isoelectric Point | 5.05 |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | N.A. |
| Description | Sargramostim (127 residue glycoprotein) is a human recombinant granulocyte macrophage colony-stimulating factor expressed in yeast system. Substitution of Leu23 leads to a difference from native protein. |
| Indication/Disease | Used to treat cancer and in bone marrow transplant |
| Pharmacodynamics | Sargramostim is used in the treatment of bone marrow transplant recipients or those exposed to chemotherapy and recovering from acute myelogenous leukemia, Leukine or GM-CSF is a hematopoietic growth factor which stimulates the survival, clonal expansion (proliferation) and differentiation of hematopoietic progenitor cells. GM-CSF is also capable of activating mature granulocytes and macrophages. After a bone marrow transplant or chemotherapy, patients have a reduced capacity to produce red and white blood cells. Supplementing them with external sources of GM-CSF helps bring the level of neutrophils back to normal so that they can better fight infections. |
| Mechanism of Action | Sargramostim binds to the Granulocyte-macrophage colony stimulating factor receptor which stimulates a JAK2 STAT1/STAT3 signal transduction pathway which leads to the production of hemopoietic cells and neutrophils |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | 420 mL/min/m2 [Normal people with liquid LEUKINE (IV)] |
| Categories | Immunosuppressive Agents |
| Patents Number | CA1341150 |
| Date of Issue | 05/12/00 |
| Date of Expiry | 05/12/17 |
| Drug Interaction | N.A. |
| Target | Granulocyte-macrophage colony-stimulating factor receptor subunit alpha,Interleukin-3 receptor subunit alpha,Cytokine receptor common subunit beta,Syndecan-2,Bone marrow proteoglycan |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Leucomax |
| Company | Novartis |
| Brand Discription | Leucomax contains a chemical which stimulates the colonies of white stem cells within the bone marrow causing the level of granulocytes in the blood to rise. Increasing the levels of granulocytes in the blood stream reduced the risk and severity of infe |
| Prescribed for | Used for reducing severe, life-threatening, or fatal infections after chemotherapy for acute myelogenous leukemia. It is also used to help increase the success of autologous bone marrow transplant and to help increase survival in patients who have bone ma |
| Chemical Name | N.A. |
| Formulation | N.A. |
| Physcial Appearnce | Solution |
| Route of Administration | Subcutaneous and Intravenous infusion |
| Recommended Dosage | In case of Intravenous Chemotherapy-induced neutropenia in adultS, 250 mcg/m2 daily for up to 42 days as required, to be given as IV infusion over 4 hr and in case of Intravenous Treatment and prevention of neutropenia in patients receiving myelosuppressivec chemotherapy. |
| Contraindication | N.A. |
| Side Effects | It is common to have aching bones and joints for 2-3 days starting 1-2 days after the start of the injections. This is usually mild and is caused by the bone marrow working harder to make white cells. Occasionally it is more troublesome and pain killers are required. |
| Useful Link | http://www.cancernet.co.uk/leucomax.htm |
| PubMed ID | 25416452, 25270293, 15583528, 25270293, 27838641, 27783330, 27576783, 27619199, 27141384 |
| 3-D Structure | Th1017 (View) or (Download) |