Cover Story: Driving cancer through ErbB3 

 

Table 1. Targeted therapies against HER2 and ErbB3. In Jaiswal et al., researchers report data suggesting that cancers driven by oncogenic mutations in epidermal growth factor receptor 3 (EGFR3; HER3; ErbB3) could respond to existing therapies against HER2 (EGFR2; ErbB2; neu). The data also further support the idea of developing ErbB3-targeting therapies to treat cancer. There are at least four HER2-targeting therapies marketed to treat various types of cancer with another five in late-stage clinical development or under regulatory review. The most advanced ErbB3-targeting therapies are in Phase II testing.

Source: BCIQ; BioCentury Archives

Company

Product

Description

Latest stage of development

Marketed and late-stage therapies that target HER2

Genentech Inc. / Chugai Pharmaceutical Co. Ltd. (Tokyo:4519) / Roche (SIX:ROG; OTCQX:RHHBY)

Herceptin trastuzumab

Humanized mAb against HER2

Marketed

Genentech Inc. / Chugai Pharmaceutical Co. Ltd. / Roche

Perjeta pertuzumab

Humanized mAb HER dimerization inhibitor that prevents HER2 from binding to other HER receptors (EGFR, ErbB3 and ErbB4)

Marketed

Genentech Inc. / Chugai Pharmaceutical Co. Ltd. / ImmunoGen Inc. (NASDAQ:IMGN) / Roche

Kadcyla ado-trastuzumab emtansine

Humanized mAb against HER2 linked to ImmunoGen's DM1 cytotoxic agent

Marketed

GlaxoSmithKline plc (LSE:GSK; NYSE:GSK) / Eddingpharm Inc.

Tykerb lapatinib

Small molecule EGFR and HER2 receptor kinase inhibitor

Marketed

Boehringer Ingelheim GmbH

Tomtovok afatinib

Small molecule dual inhibitor of EGFR, HER2 and ErbB4 (HER4)

Registration

Biocon Ltd. (NSE:BIOCON; BSE:BIOCON) /
Mylan Inc. (NASDAQ:MYL)

Biosimilar trastuzumab

Humanized mAb against HER2

Phase III

Celltrion Inc. (KOSDAQ:068270) /
Nippon Kayaku Co. Ltd.
(Tokyo:4272)

CT-P6

Humanized mAb against HER2

Phase III

Pfizer Inc. (NYSE:PFE) / SFJ Pharmaceuticals Inc.

Dacomitinib

Small molecule inhibitor of human EGFR, HER2 and ErbB4

Phase III

Symphony Evolution Inc. / Exelixis Inc. (NASDAQ:EXEL) / Kadmon Corp. LLC

XL647; KD019

Spectrum selective small molecule inhibitor of EGFR, HER2 and VEGF

Phase III

Clinical-stage therapies that target ErbB3

Genentech Inc. / Roche

MEHD7945A

Humanized IgG1 mAb targeting EGFR and ErbB3

Phase II

Merrimack Pharmaceuticals Inc. (NASDAQ:MACK) / Sanofi (Euronext:SAN; NYSE:SNY)

MM-121

Human mAb against ErbB3

Phase II

Merrimack Pharmaceuticals Inc.

MM-111

Bispecific antibody targeting HER2 and ErbB3

Phase II

Daiichi Sankyo Co. Ltd. (Tokyo:4568; Osaka:4568) / Amgen Inc. (NASDAQ:AMGN)

U3-1287, AMG 888

Human mAb against ErbB3

Phase I/II

Aveo Pharmaceuticals Inc. (NASDAQ:AVEO)

AV-203

ErbB3-targeted antibody

Phase I

Merrimack Pharmaceuticals Inc.

MM-141

Tetravalent antibody targeting insulin-like growth factor 1 receptor (IGF1R; CD221) and ErbB3

Phase I

Novartis AG (NYSE:NVS; SIX:NOVN) /
MorphoSys AG (Xetra:MOR; Pink:MPSYF)

LJM716

Human HuCAL antibody against ErbB3

Phase I

Regeneron Pharmaceuticals Inc. (NASDAQ:REGN)

REGN1400

Human ErbB3 antibody

Phase I

Roche

RG7116

Anti-HER3/ADCC mAb

Phase I

Zensun (Shanghai) Sci. & Tech. Co. Ltd.

rhErbB3-f

Recombinant human ErbB3 fragment vaccine

Phase I