Balixafortide

Summary

Balixafortide (POL6326) is a potent, selective bicyclic peptide CXCR4 antagonist developed by Polyphor AG. It is being investigated primarily in combination with eribulin for the treatment of HER2-negative metastatic breast cancer, exploiting the CXCR4/CXCL12 axis involved in tumor homing and metastasis. It has also been explored for hematopoietic stem cell mobilization.

Mechanism of Action

Selectively antagonizes CXCR4 (C-X-C chemokine receptor type 4), blocking SDF-1/CXCL12-mediated signaling, thereby inhibiting tumor cell migration, metastasis, and mobilizing hematopoietic stem cells from bone marrow into peripheral blood.

Routes of Administration

Goals & Uses

• Hematopoietic stem cell mobilizationHematologyModerate
• Anti-tumor activity in HER2-negative metastatic breast cancerOncologyModerate
• Inhibition of tumor metastasis via CXCR4 blockadeOncologyModerate
• Sensitization of tumors to chemotherapyOncologyLow

Contraindications

• Severe hepatic impairmentOrganModerateLiver function concerns
• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Hypersensitivity to balixafortide or excipientsAllergyHigh

Adverse Effects

• LeukocytosisHematologicUncommon
• HeadacheNeurologicUncommonPain in the head or upper neck
• HypotensionCardiovascularUncommonLow blood pressure
• NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
• FatigueGeneralCommonLow energy or tiredness
• Infusion-related reactionsHypersensitivityCommon

Drug Interactions

• EribulinLow
• CYP3A4 substratesLow
• Other CXCR4 antagonists (e.g., plerixafor)Moderate

Population Constraints

• Patients with active autoimmune conditionsImmunologicRelative
• Pediatric patientsAgeRelative
• Pregnant womenReproductiveAbsolute
• Patients with severe renal impairmentOrgan ImpairmentRelative

Regulatory Status

• European UnionInvestigationalNo EMA marketing authorization; clinical trials conducted in Europe under Polyphor AG sponsorship.
• United StatesInvestigationalNo FDA approval; investigated under IND for metastatic breast cancer and HSC mobilization.
• United KingdomInvestigationalNot approved by MHRA; investigational status only.

Not approved by any regulatory authority as of the knowledge cutoff. Investigated in Phase II clinical trials for HER2-negative metastatic breast cancer in combination with eribulin. Orphan Drug Designation has not been widely reported for this compound.

Evidence & Sources

No sources recorded yet.