FUSION PROTEINS: APPLICATIONS AND CHALLENGES - Fusion Protein Technologies for Biopharmaceuticals: Applications and Challenges - page 16

TABLE 1.1 Competition Between Antibodies and Fusion Proteins that Capture TNF-a

Sales 2009 a Sales 2010 a Sales 2011 a

Drug Approval Components Manufacturing Dosing

Remicade 1 08/1998 Chimeric mAb Continuous perfusion

in CHO

IV 2-4 weekly 5.9 7.3 8.5

Enbrel 1 11/1998 Receptor Fc fusion Fed-batch in CHO SC 1-2 weekly 6.3 7.4 7.9

Humira 1

01/2003 Fully human mAb Extended

fed-batch in CHO

SC bi-weekly 5.5 6.7 7.9

Cimzia 1 04/2008 PEGylated

humanized Fab

Fed-batch E. coli SC bi-weekly 0.11 0.26 0.31

Simponi 1 04/2009 Fully human mAb Perfusion in Sp2/0 SC monthly 0.11 0.32 0.67

a Global sales in billion $.

biological drugs increased by 17% in 2010. Splitting the
sales up, it can be seen that the growth rate of proteins was
15%, whereas antibody sales expanded by 21%. This
means that of the $15.91 billion growth antibodies con-
tributed 55% and protein 45%. Another important obser-
vation is the higher approval success rate of 32% for
biological compared to 13% for small molecules between
1993 and 2004 [172]. In Figure 1.4, the annual sales of
important therapeutic protein classes in the United States
are presented.

Although the growth of fusion protein sales has been
relatively modest in comparison to mABs or hormones,
there is a huge potential for this molecule class as can be
seen in a much deeper analysis in Chapter 2.

1.8 CONCLUSION AND FUTURE PERSPECTIVE

During the last decades, human imagination has assembled
a plethora of new protein combinations from the vast array

TABLE 1.2 Mergers and Acquisitions Involving Companies with Fusion Protein Technology

Value
($ Million) Technology

Phase
(at Acquis.) Buyer Target Date Fusion Protein Indication

Alexion Enobia 07/02/2012 610 Bone targeting ENB-0040 Hypophosphatasia II

Alexion Taligen 31/01/2011 111 C3d targeting TT30 Autoimmune Preclin.

Insys Neopharm 29/10/2010 135 Immunotoxins NK-408 Oncology III

Bristol-Myers
Squibb

Zymogenetics 07/09/2010 885 Fc fusion Atacicept Autoimmune II

Biomarin Zystor 07/09/2010 22 GILT ZC-701 Pompe's disease I

Emergent Trubion 18/08/2010 97 SMIP and

Scorpion

SBI-087
TRU-016

Autoimmune
Oncology

II

Teva CoGenesys 12/08/2010 400 Albumin fusion Neugranin

Cardeva

Febrile neutropenia
Congestive
heart failure

II
II

Pfizer CovX 22/01/2008 n.a. CovX body

(peptide-
mAb fusion)

CVX-045
CVX-060
CVX-096

Oncology
Oncology
Type 2 diabetes

I
II

Topotarget Apoxis 18/12/2007 19 Mega Ligand APO010 Oncology I

Pfizer Biorexis 11/04/2007 n.a. Transferrin

fusion

BRX-0585 Type 2 diabetes Preclin.

Biogen Idec Syntonix 01/02/2007 40 Monomeric Fc

fusion

FIX-Fc Hemophilia B IND

Amgen Avidia 29/09/2006 290 Avimer

(modular
binding
domains)

IL-6
inhibitor

Inflammation,
autoimmune

I

Medigene Avidex 31/08/2006 62 TCR technology EsoDex Oncology Preclin.

GILT, glycosylation independent lysosomal targeting; SMIP, small modular immunopharmaceutical; TCR, T-cell receptor.