Sargramostim
Recombinant GM-CSF myeloid growth factor for neutropenia and stem cell mobilization in transplant settings.
Chemical Identity
| Property | Value |
|---|---|
| Molecular Weight | ~14-30 kDa |
| Gene | CSF2 |
| Receptor | CSF2RA/CSF2RB |
| CAS Number | 123774-72-1 |
| Route | IV, SC |
Structure
Sargramostim (Leukine) is recombinant human GM-CSF produced in yeast. The 127-amino acid protein has glycosylation patterns differing from native human GM-CSF due to yeast expression system, but retains full biological activity through the GM-CSF receptor.
Mechanism of Action
GM-CSF binds its receptor on myeloid progenitors, activating JAK2/STAT5 signaling. This stimulates proliferation and differentiation of granulocytes, monocytes, and macrophages. GM-CSF also enhances phagocytic function and antigen presentation.
Clinical Applications
- Autologous transplant: Myeloid reconstitution
- Allogeneic transplant: Engraftment acceleration
- AML induction: Myeloid recovery after chemotherapy
- Radiation injury: Hematopoietic syndrome treatment
Pharmacokinetics
- Half-life: 1-2 hours (IV), 2-3 hours (SC)
- Bioavailability: 60-80%
- Route: IV, SC
- Dosing: 250 mcg/m2/day
Safety and Side Effects
Bone pain, fever, fluid retention, capillary leak syndrome (high doses), and allergic reactions. More inflammatory side effects than G-CSF.
References
- Nemunaitis, J. (1993). GM-CSF after autologous bone marrow transplant. Journal of Clinical Oncology, 11, 1643-1651.
- Armitage, J.O. (1998). Applications of GM-CSF. Blood, 92, 4491-4508.
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