Balixafortide
DRACPC ID DRACPC0050
Active Ingredients Balixafortide
Description An orally bioavailable inhibitor of CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell-mobilization activities. Balixafortide binds to the chemokine receptor CXCR4, thereby preventing the binding of stromal derived factor-1 (SDF-1 or CXCL12) to the CXCR4 receptor and subsequent receptor activation. This may induce the mobilization of hematopoietic stem and progenitor cells from the bone marrow into blood. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types; CXCL12/CXCR4 interaction induces retention of hematopoietic cells in the bone marrow.
Synonyms POL6326; Ala-cys-ser-ala-pro-arg-tyr-cys-tyr-gln-lys-pro-pro-tyr-his Cyclic (2->9)-disulfide; Balixafortide
Type Biotech
Disease Breast Cancer
Classification
CXCR4 inhibitor Peptide and derivative Cyclic
Structure Information
Molecular Formula C84H118N24O21S2
Molecular Weight 1864.1
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name 3-[(1R,4S,7S,10S,16S,22R,25S,28S,31S,34R,37S,40S,43S,46R,52S,55S)-25-(4-aminobutyl)-43-(2-aminoethyl)-40-(3-carbamimidamidopropyl)-55-(hydroxymethyl)-10,31,37-tris[(4-hydroxyphenyl)methyl]-7-(1H-imidazol-5-ylmethyl)-4,52-dimethyl-3,8,11,17,23,26,29,32,35,38,39,42,45,51,54,57-hexadecaoxo-59,60-dithia-2,5,6,9,12,18,24,27,30,33,36,41,44,50,53,56-hexadecazapentacyclo[32.23.4.012,16.018,22.046,50]henhexacontan-28-yl]propanamide
InChI InChI=1S/C84H118N24O21S2/c1-44-70(116)102-62-41-130-131-42-63(77(123)98-57(35-46-14-20-50(110)21-15-46)69(115)68(114)53(10-5-31-91-84(88)89)94-73(119)56(28-30-86)97-79(125)64-11-6-32-106(64)81(127)45(2)93-76(122)61(40-109)101-78(62)124)103-74(120)58(36-47-16-22-51(111)23-17-47)99-72(118)55(26-27-67(87)113)95-71(117)54(9-3-4-29-85)96-80(126)65-12-7-33-107(65)83(129)66-13-8-34-108(66)82(128)60(37-48-18-24-52(112)25-19-48)100-75(121)59(105-104-44)38-49-39-90-43-92-49/h14-25,39,43-45,53-66,104-105,109-112H,3-13,26-38,40-42,85-86H2,1-2H3,(H2,87,113)(H,90,92)(H,93,122)(H,94,119)(H,95,117)(H,96,126)(H,97,125)(H,98,123)(H,99,118)(H,100,121)(H,101,124)(H,102,116)(H,103,120)(H4,88,89,91)/t44-,45-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64+,65+,66-/m0/s1
InChI_Key OYWQJZAVFWOOBF-WBMPNIIXSA-N
SMILES C[C@@H]1NN[C@H](C(N[C@H](C(N2CCC[C@H]2C(N3CCC[C@@H]3C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H]4CSSC[C@@H](C(N[C@H](C(N[C@H](C(N5CCC[C@@H]5C(N[C@H](C(N[C@H](C(C([C@@H](NC4=O)CC6=CC=C(C=C6)O)=O)=O)CCCNC(N)=N)=O)CCN)=O)=O)C)=O)CO)=O)NC1=O)=O)CC7=CC=C(C=C7)O)=O)CCC(N)=O)=O)CCCCN)=O)=O)=O)CC8=CC=C(C=C8)O)=O)CC9=CN=CN9
External Codes
PubChem CID 138752609
DrugBank Accession Number DB15370
NCI Thesaurus Code C91094
UNII PRC974M49B GSRS
CAS 1051366-32-5
Drug approval
Drug indication
Investigated for use/treatment in locally recurrent/metastatic/advanced breast cancer.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT04826016 | A Phase Ib/II Study to Optimize POL6326 (Balixafortide) in Combination With Nab-paclitaxel or Eribulin in Patients With HER2-negative Advanced Breast Cancer | Advanced Breast Cancer | Phase 1/2 | Treatment |
| NCT01837095 | A Phase I Dose Escalation Study of POL6326 With Eribulin in Patients With Relapsed, Triple Negative and Hormone Refractory ER Positive Metastatic Breast Cancer | Metastatic Breast Cancer | Phase 1 | Treatment |
| NCT01413568 | A Phase I/II Study Evaluating the Safety and Efficacy of Intravenous POL6326 for the Mobilization and Transplantation of HLA-Matched Sibling Donor Hematopoietic Stem Cells in Patients With Advanced Hematological Malignancies | Acute Myeloid Leukemia in Remission; Adult Acute Lymphoblastic Leukemia in Remission; Chronic Myelogenous Leukemia (CML); Non-Hodgkin's Lymphoma (NHL) or Hodgkin's Disease (HD) in 2nd or Greater Complete Remission, Partial Remission; Chronic Lymphocytic Leukemia (CLL); Multiple Myeloma (MM); Myelodysplastic Syndrome (MDS); Myeloproliferative Disorders | Phase 1/2 | Treatment |
| NCT03786094 | An International, Phase 3, Multicenter, Randomized, Open- Label Trial Comparing Balixafortide in Combination With Eribulin Versus Eribulin Alone in Patients With HER2 Negative, Locally Recurrent or Metastatic Breast Cancer | Metastatic Breast Cancer; Locally Recurrent Breast Cancer | Phase 3 | Treatment |
| NCT01905475 | CXCR4 AnTagonism for Cell Mobilisation and Healing in Acute Myocardial Infarction (CATCH-AMI). A Phase IIa, Double-Blind, Placebo-Controlled, Randomised, Multi-centre Study of POL6326, a CXCR4 Antagonist, in Patients With Large Reperfused ST Elevation Myocardial Infarction | Large Reperfused ST-Elevation Myocardial Infarction | Phase 2 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
