pegaptanib
Trade name: macugen
Approved
Sep 17, 2004
Pegaptanib is a selective vascular endothelial growth factor (VEGF) antagonist indicated for the treatment of neovascular (wet) age-related macular degeneration. Pegaptanib is an aptamer, a pegylated modified single-stranded oligonucleotide, which adopts a threedimensional conformation that enables it to bind to extracellular VEGF. Pegaptanib specifically binds to the 165 isoform of VEGF, a protein that plays a critical role in angiogenesis (the formation of new blood vessels) and increased permeability (leakage from blood vessels), two of the primary pathological processes responsible for the vision loss associated with neovascular age-related macular degeneration. Pegaptanib is administered in a 0.3 mg dose once every six weeks by intravitreal injection. An intravitreal injection is one that is administered directly into the eye, more specifically, into the vitreous humour, or the jelly-like fluid within the eye. — NCATS
Clinical trial activity
39 trials · 23 clinical orgs · 3 marketing orgs
Earliest trial started May 1, 2001 (NCT00321997)
Timeline
2000s
- Jan 1, 2001
Eyetech Pharmaceuticals — Earliest Phase 2 Sponsor(trial)
- Jan 1, 2003
Earliest Phase 1 Sponsor(trial)
- Jan 1, 2004
Earliest Phase 3 Sponsor(trial)
- Sep 17, 2004
Earliest FDA Approval
- Sep 17, 2004
Bausch & Lomb — Marketing Organization
- Sep 17, 2004
Bausch Health Companies — NDA Secondary Org
- Sep 17, 2004
Bausch & Lomb — NDA Secondary Org
- Dec 17, 2004
Eyetech Pharmaceuticals — First NDA Organization
- Dec 17, 2004
Eyetech Pharmaceuticals — NDA Organization
Indications
Studied for
- Choroidal Neovascularization · Phase 3
- Diabetes Mellitus · Phase 3
- Diabetes Mellitus, Type 1 · Phase 2
- Diabetes Mellitus, Type 2 · Phase 2
- Diabetic Retinopathy · Phase 4
- Drugs, Investigational · Phase 3
- Glaucoma, Neovascular · Phase 1
- Macula Lutea · Phase 4
- Macular Degeneration · Phase 4
- Macular Edema · Phase 4
- Neovascularization, Pathologic · Phase 4
- Retinal Diseases · Phase 3
- Retinal Vein Occlusion · Phase 4
- von Hippel-Lindau Disease · Phase 1
Mechanism of action
- Vascular endothelial growth factor AANTAGONIST
VEGFA antagonist
It's an aptamer, a pegylated modified oligonucleotide
Selective
- Vascular endothelial growth factor AINHIBITOR
Vascular endothelial growth factor A inhibitor
Approval history
- approvedPriority reviewSep 17, 2004
Chemistry & pharmacology
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- Yes
- Delivery
- Parenteral
- Availability
- Discontinued
- Multi-specific
- No
Oral
No
Parenteral
Yes
Topical
No
Sources
- WikipediaPegaptanib ↗
- NCATS2H1PA8H1EN ↗
- ChEMBLCHEMBL2108752 ↗
- ChEMBLCHEMBL1201421 ↗
Also known as
- eye001
- eye001
- eye001
- eye 001
- eye 001
- eyeoo1
- eyeoo1
- macugen
- macugen
- macugen
- macugen
- macugen
- nx1838
- nx1838
- nx1838
- nx1838
- nx 1838
- nx 1838
- pegaptanib
- pegaptanib
- pegaptanib
- pegaptanib
- pegaptanib
- pegaptanib
- pegaptanib
- pegaptanib
- pegaptanib
- pegaptanib octasodium
- pegaptanib octasodium
- pegaptanib octasodium
- pegaptanib octasodium
- pegaptanib sodium
- pegaptanib sodium
- pegaptanib sodium
- pegaptanib sodium
- pegaptanib sodium
- pegaptanib sodium
- pegaptanib sodium
- pegaptanib sodium
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02321267 | Phase 4 | Dec 1, 2014 | Kagawa University |
| NCT01589718 | Phase 3 | Apr 1, 2012 | Greater Houston Retina Research |
| NCT01487044 | N/A | Dec 5, 2011 | Eyetech Pharmaceuticals, Retina Institute of Hawaii |
| NCT01487070 | Phase 1 | Apr 1, 2011 | Retina Institute of Hawaii |
| NCT01175070 | Phase 4 | Jan 1, 2011 | Pfizer, University of Oxford |
| NCT01189461 | Phase 3 | Jan 1, 2011 | Pfizer |
| NCT01218230 | N/A | Dec 1, 2010 | L. V. Prasad Eye Institute, Pfizer |
| NCT01100307 | Phase 3 | May 1, 2010 | Pfizer |
| NCT01573572 | Phase 4 | Apr 1, 2010 | Bausch Health Companies |
| NCT01281098 | Phase 2 | Mar 1, 2010 | Association for Innovation and Biomedical Research on Light and Image (AIBILI) |
| NCT01486238 | Phase 4 | Apr 1, 2009 | Gulf Coast Eye Institute |
| NCT00790803 | N/A | Mar 1, 2009 | Wake Forest University |
| NCT00788177 | Phase 3 | Nov 1, 2008 | Pfizer, University of Heidelberg |
| NCT00709657 | N/A | Mar 1, 2008 | University of Vienna |
| NCT01486771 | Phase 4 | Nov 1, 2007 | Gulf Coast Eye Institute, Pfizer |
| NCT00446381 | N/A | Oct 1, 2006 | McMaster University, Pfizer, University of Western Ontario |
| NCT00327470 | Phase 4 | Jul 1, 2006 | Pfizer |
| NCT00358423 | Phase 1/Phase 2 (Phase 2) | Jul 1, 2006 | Eyetech Pharmaceuticals, Johns Hopkins University |
| NCT00531336 | Phase 2 | Jul 1, 2006 | Ludwig Boltzmann Institute |
| NCT00324116 | Phase 4 | Jul 1, 2006 | Pfizer |
Organizations
Research & Development (23)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 22 | 7 | 4 | 2001 |
| Eyetech Pharmaceuticals | For profit | 15 | 10 | 5 | 2001 |
| Gulf Coast Eye Institute | Academic/Hospital | 2 | 2 | 1 | 2007 |
| Johns Hopkins University | Academic/Hospital | 2 | 2 | 1 | 2006 |
| Retina Institute of Hawaii | Academic/Hospital | 2 | 2 | 2 | 2011 |
| Association for Innovation and Biomedical Research on Light and Image (AIBILI) | Academic/Hospital | 1 | 1 | 1 | 2010 |
| Barnes Retina Institute | Academic/Hospital | 1 | 1 | 1 | 2006 |
| Bausch Health Companies | For profit | 1 | 1 | 1 | 2010 |
| Greater Houston Retina Research | Academic/Hospital | 1 | 1 | 1 | 2012 |
| Hermann Eye Center | Academic/Hospital | 1 | 1 | 1 | 2006 |
| Kagawa University | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Ludwig Boltzmann Institute | Academic/Hospital | 1 | 1 | 1 | 2006 |
| L. V. Prasad Eye Institute | Academic/Hospital | 1 | 1 | 1 | 2010 |
| McMaster University | Academic/Hospital | 1 | 0 | 1 | 2006 |
| National Eye Institute (NEI) | Government | 1 | 1 | 1 | 2003 |
| Novartis | For profit | 1 | 1 | 1 | 2005 |
| Novelion Therapeutics | For profit | 1 | 0 | 1 | 2005 |
| Palmetto Retina Center | Academic/Hospital | 1 | 1 | 1 | 2006 |
| University of Heidelberg | Academic/Hospital | 1 | 1 | 1 | 2008 |
| University of Oxford | Academic/Hospital | 1 | 1 | 1 | 2011 |
Marketing (4)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Bausch & Lomb | For profit | MKTG | Sep 17, 2004 |
| Bausch & Lomb | For profit | NDA2 | Sep 17, 2004 |
| Bausch Health Companies | For profit | NDA2 | Sep 17, 2004 |
| Eyetech Pharmaceuticals | For profit | NDA | Dec 17, 2004 |