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motixafortide (Aphexda)
Indications:
- for use in combination with filgrastim to mobilize hematopoietic stem cells to the peripheral blood for collection & subsequent autologous hematopoietic stem cell transplantation in patients with multiple myeloma
Contraindications:
- pregnancy (potential risk to fetus)
Dosage:
- filgrastim 10 ug/kg SC QD for 4 days prior to 1st dose of motixafortide & on each day prior to apheresis
- premedicate with diphenhydramine, famotidine, montelukat & acetaminophen
- motixafortide 1.25 mg/kg SC over 2 minutes 10-14 hours prior to the 1st apheresis
- a 2nd dose 10-14 hours prior to the 3rd apheresis
Pharmacokinetics:
- peak plasma time: 0.25-1.17 hr
- >99% protein bound
- volume of distribution: 27 liter
- metabolized into small peptides & individual amino acids
- catabolism may occur in both blood & hepatic microsomes
- no ative metabolites
- elimination 1/2 life: ~2 hr
Adverse effects:
- injection-site pain (53%), erythema (27%), pruritus (24%)
- pruritus (38%)
- flushing (33%)
- back pain (21%)
- paresthesia (19%)
- rash (16%)
- hypokalemia (15%)
- nausea (14%)
- urticaria (14%)
- erythema (12%)
- exfoliative generalized dermatitis (<10%)
- ear swelling (<10%)
- pyrexia (<10%), chills (<10%)
- dizziness (<10%)
- tremor (<10%)
- hypertension (<10%)
Mechanism of action:
- inhibits C-X-C motif chemokine receptor 4 (CXCR4) blocks binding of its cognate ligand, stromal-derived factor 1-alpha/ C-X-C motif chemokine ligand 12 (SDF-1alpha/CXCL12)
- SDF-1alpha& CXCL12 play a role in trafficking & homing of hematopoietic stem cells to the marrow compartment
General
hematologic agent
Database Correlations
PUBCHEM cid=91865076
References
- motixafortide (Rx)
https://reference.medscape.com/drug/aphexda-motixafortide-4000336