Brolucizumab

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Brolucizumab
Monoclonal antibody
TypeSingle-chain variable fragment
SourceHumanized
TargetVEGFA
Clinical data
SynonymsESBA1008, RTH258
Routes of
administration
Intravitreal
ATC code
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC1164H1768N310O372S7
Molar mass26.31 kDa g·mol−1

Brolucizumab (INN) is a humanized single-chain antibody fragment designed for the treatment of wet age-related macular degeneration.[1][2]

This drug was developed by ESBATech (discovery to phase 2a), Alcon Laboratories (phase 2b) and Novartis (phase 3).

Laboratory development names are RTH258 (Novartis Compound Code) and ESBA1008 (ESBATech AG).

Brolucizumab successfully completed phase 3 development in wet age-related macular degeneration (AMD) meeting the primary efficacy endpoint of non-inferiority to aflibercept in mean change in best corrected visual acuity (BCVA) from baseline to week 48. Furthermore, brolucizumab demonstrated superiority to aflibercept in key secondary endpoint measures of disease activity in wet AMD, a leading cause of blindness in two head-to-head pivotal Phase III studies.

Whilst brolucizumab was initially developed for ophthalmology, non-ophthalmology indications (to which Cell Medica hold development rights) are also under investigation, under the name DLX1008. DLX1008 is under preclinical development for Kaposi sarcoma[3] and glioblastoma.[4]

References[edit]

  1. ^ Statement On A Nonproprietary Name Adopted By The USAN Council - Brolucizumab, American Medical Association.
  2. ^ World Health Organization (2014). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 112" (PDF). WHO Drug Information. 28 (4).
  3. ^ Eason, Anthony B.; Sin, Sang-Hoon; Szabó, Emese; Phillips, Douglas J.; Droste, Miriam; Shamshiev, Abdijapar; Dittmer, Dirk P.; Weller, Michael (2018). "Abstract 4: Antitumor activity of DLX1008, a single chain antibody fragment binding to VEGF-A, in in vivo preclinical models of Kaposi sarcoma and glioblastoma". Cancer Research. 78 (13 Supplement): 4–4. doi:10.1158/1538-7445.AM2018-4. ISSN 0008-5472.
  4. ^ Szabó, Emese; Phillips, Douglas J.; Droste, Miriam; Marti, Andrea; Kretzschmar, Titus; Shamshiev, Abdijapar; Weller, Michael (2018). "Antitumor Activity of DLX1008, an Anti-VEGFA Antibody Fragment with Low Picomolar Affinity, in Human Glioma Models". Journal of Pharmacology and Experimental Therapeutics. 365 (2): 422–429. doi:10.1124/jpet.117.246249. ISSN 0022-3565.