EGFR antagonists(Epidermal growth factor receptor erbB1 antagonists), HER2 exon 20 inhibitors(ERBB2 Exon 20 Mutation inhibitors), HER3 antagonists(Receptor tyrosine-protein kinase erbB-3 antagonists)

+ [1]

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

Receptor BioLogix, Inc.

Active Organization-

Inactive Organization

Receptor BioLogix, Inc.

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

100 Clinical Results associated with RB-200

100 Translational Medicine associated with RB-200

100 Patents (Medical) associated with RB-200

Literatures (Medical) associated with RB-200

01 Oct 2008·Molecular Cancer TherapeuticsQ2 · MEDICINE

Human epidermal growth factor receptor (HER-1:HER-3) Fc-mediated heterodimer has broad antiproliferative activityin vitroand in human tumor xenografts

Q2 · MEDICINE

Article

Author: Jorgensen, Brett ; Turin, Lisa ; Ni, Irene ; Sarup, Jay ; Bai, Xiaomei ; Brdlik, Cathleen ; Lindley, Peter ; Higaki, Jeffrey N. ; Jin, Pei ; Liu, Jim ; Shepard, H. Michael ; Rozzelle, James ; Beryt, Malgorzata ; Zhang, Juan ; Kumari, Rajendra ; Watson, Susan A. ; Lau, Francis W.

AbstractAll four members of the human epidermal growth factor (EGF) receptor (HER) family are implicated in human cancers. Although efficacious in a subset of patients, resistance to single-targeted anti-HER therapy [i.e., cetuximab (Erbitux) and trastuzumab (Herceptin)] is often associated with coexpression of other HER family members. This may be overcome by a HER ligand binding molecule that sequesters multiple EGF-like ligands, preventing ligand-dependent receptor activation. Toward this end, we have combined the HER-1/EGFR and HER-3 ligand binding domains, dimerized with fusion of an Fc fragment of human IgG1. This resulted in a mixture of HER-1/Fc homodimer (HFD100), HER-3/Fc homodimer (HFD300), and HER-1/Fc:HER-3/Fc heterodimer (RB200), also termed Hermodulins. The purified first-generation RB200 bound EGF and neuregulin 1 (NRG1)-β1 ligands, determined by cross-linking and direct binding studies. The binding affinity for both was ∼10 nmol/L by dissociation-enhanced lanthanide fluorescence immunoassay using europium (Eu)-labeled ligands. Competition studies with RB200 using Eu-EGF or Eu-NRG1-β1 revealed that RB200 bound HER-1 ligands, including transforming growth factor-α and heparin-binding EGF, and HER-3 ligands NRG1-α and NRG1-β3. RB200 inhibited EGF- and NRG1-β1–stimulated tyrosine phosphorylation of HER family proteins, proliferation of a diverse range of tumor cells in monolayer cell growth assays, tumor cell proliferation as a single agent and in synergy with tyrosine kinase inhibitors, lysophosphatidic acid–stimulated cell proliferation, and tumor growth in two human tumor xenograft nude mouse models. Taken together, the data reveal that RB200 has the potential to sequester multiple HER ligands and interfere with signaling by HER-1, HER-2, and HER-3. [Mol Cancer Ther 2008;7(10):3223–36]

01 May 2006·Scientific AmericanQ4 · CROSS-FIELD

Blockbuster Dreams

Q4 · CROSS-FIELD

Article

Author: Stix, Gary

A brief account on the properties of Herceptin and Dimercept, particularly on their application in cancer therapy, is presented.New understanding of the biol. behind a successful cancer therapy may lead to a drug that can treat an array of solid tumors.

10 Apr 2003·FEBS LettersQ3 · BIOLOGY

Selective cytotoxicity following Arg‐to‐Lys substitution in tritrpticin adopting a unique amphipathic turn structure

Q3 · BIOLOGY

Article

Author: Chul Won Lee ; Jae Il Kim ; Yong Chul Kim ; Kyung Soo Hahm ; Sung Tae Yang ; Song Yub Shin

In antimicrobial peptides, the cationic property due to basic amino acids has been widely recognized as an important factor to promote electrostatic interaction with negatively charged phospholipids. However, little is known about the differences between two basic residues, Arg and Lys, in membrane binding affinity. Tritrpticin is an Arg‐ or Trp‐rich antimicrobial peptide with a broad spectrum of antibacterial and antifungal activity. To investigate the structural and functional differences between Arg and Lys residues, here we designed and synthesized Arg‐containing peptides, tritrpticin and SYM11, and their counterpart Lys‐substituted peptides, TRK and SYM11KK, respectively. Although there were no remarkable conformational differences between Arg‐containing and Lys‐substituted peptides, TRK and SYM11KK exhibited almost two‐fold enhanced antibacterial activity but significantly reduced hemolytic activity as compared to tritrpticin and SYM11, respectively. Furthermore, Arg‐containing peptides showed strong binding affinity to both zwitterionic and anionic liposomes, whereas Lys‐substituted peptides interacted weakly with zwitterionic liposomes but strongly with anionic liposomes. These results suggest that the primary amine of Lys interacts less electrostatically with zwitterionic phospholipids than the guanidinium group of Arg. Our results obtained in this study may be helpful in the design of drugs that target negatively charged phospholipids.

100 Deals associated with RB-200

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Discovery	US	Receptor BioLogix, Inc.	-

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