Motixafortide
Trade name: Aphexda
Approved
Sep 8, 2023
A CXCR4 antagonist is a substance which blocks the CXCR4 receptor and prevent its activation. Blocking the receptor stops the receptor's ligand, CXCL12, from binding which prevents downstream effects. CXCR4 antagonists are especially important for hindering cancer progression because one of the downstream effects initiated by CXCR4 receptor activation is cell movement which helps the spread of cancer, known as metastasis. The CXCR4 receptor has been targeted by antagonistic substances since being identified as a co-receptor in HIV and assisting the development of cancer. Macrocyclic ligands have been utilised as CXCR4 antagonists. — Wikipedia
Clinical trial activity
10 trials · 12 clinical orgs · 1 marketing orgs
Earliest trial started Jul 5, 2017 (NCT03193190)
Timeline
2010s
- Jul 6, 2012
Orphan Drug Designation
- Jan 1, 2017
Earliest Phase 1 Sponsor(trial)
- Jan 1, 2018
BioLineRx, Ltd. — Earliest Phase 3 Sponsor(trial)
2020s
- Jan 1, 2021
Earliest Phase 2 Sponsor(trial)
- Sep 8, 2023
BioLineRx, Ltd. — Earliest FDA Approval
- Sep 8, 2023
BioLineRx, Ltd. — Marketing Organization
- Sep 8, 2023
BioLineRx, Ltd. — NDA Organization
Indications
Mechanism of action
- Unspecified targetAGONIST
agonist
- C-X-C chemokine receptor type 4ANTAGONIST
C-X-C chemokine receptor type 4 antagonist
Approval history
- approvedSep 8, 2023
Chemistry & pharmacology
SMILES
N=C(N)NCCC[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N1)C(N)=O- Mol. weight
- 2159.56 g/mol
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Availability
- Prescription Only
- Multi-specific
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaCXCR4 antagonist ↗
- ChEMBLCHEMBL5095449 ↗
- ChEMBLCHEMBL5095030 ↗
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07101445 | Phase 4 | Sep 24, 2025 | Emory University, Gamida Cell, National Cancer Institute (NCI) |
| NCT06442761 | Phase 1 | Dec 31, 2024 | BioLineRx, Ltd., St. Jude Children's Hospital |
| NCT06547112 | Phase 1 | Oct 31, 2024 | BioLineRx, Ltd., Washington University in St. Louis |
| NCT06514508 | Phase 3 | Sep 30, 2024 | Guangzhou Gloria Biosciences Co., Ltd. |
| NCT05618301 | Phase 1 | Mar 31, 2023 | BioLineRx, Ltd., Washington University in St. Louis |
| NCT04543071 | Phase 2 | Aug 30, 2021 | BioLineRx, Ltd., Columbia University, Regeneron |
| NCT05293171 | Phase 1 | Jun 11, 2021 | BioLineRx, Ltd., Celerion |
| NCT03246529 | Phase 3 | Jan 18, 2018 | BioLineRx, Ltd., Washington University in St. Louis |
| NCT03281369 | Phase 1/Phase 2 (Phase 2) | Oct 13, 2017 | Halozyme Therapeutics, Roche |
| NCT03193190 | Phase 1/Phase 2 (Phase 2) | Jul 5, 2017 | Roche |
Organizations
Research & Development (12)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| BioLineRx, Ltd. | For profit | 6 | 2 | 3 | 2018 |
| Washington University in St. Louis | Academic/Hospital | 3 | 2 | 2 | 2018 |
| Roche | For profit | 2 | 2 | 1 | 2017 |
| Celerion | For profit | 1 | 0 | 1 | 2021 |
| Columbia University | Academic/Hospital | 1 | 1 | 1 | 2021 |
| Emory University | Academic/Hospital | 1 | 1 | 1 | 2025 |
| Gamida Cell | For profit | 1 | 0 | 1 | 2025 |
| Guangzhou Gloria Biosciences Co., Ltd. | For profit | 1 | 1 | 1 | 2024 |
| Halozyme Therapeutics | For profit | 1 | 0 | 1 | 2017 |
| National Cancer Institute (NCI) | Government | 1 | 0 | 1 | 2025 |
| Regeneron | For profit | 1 | 0 | 1 | 2021 |
| St. Jude Children's Hospital | Academic/Hospital | 1 | 1 | 1 | 2024 |
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| BioLineRx, Ltd. | For profit | MKTG | Sep 8, 2023 |
| BioLineRx, Ltd. | For profit | NDA | Sep 8, 2023 |