A candidate targeting molecule of insulin-like growth factor-I receptor for gastrointestinal cancers

Table 1 Type I insulin-like growth factor receptor targeting agents

Class	Name	Company	Other targets than IGF-IR	Clinical study	Target organs of GI	Target organs other than GI
Inhibition of IGF-IR expression	Antisense oligonucleotide
	Antisense RNA
	siRNA
Antibodies for IGF-IR	Figitumumab (CP-751,871)1	Pfizer		Phase III	Colon	Lung, head and neck, breast, prostate, sarcoma, advanced solid tumor
	SCH 717454 (19D12)1	Schering-Plough		Phase II	Colon	sarcoma, advanced solid tumor
	IMC-A121	ImClone Systems		Phase II	Colon, HCC, pancreas, islet cell cancer	Lung, head and neck, breast, prostate, kidney, thymic, adrenocortical, sarcoma, advanced solid tumor, CMPD, leukemia, lymphoma
	R1507 (RG1507)1	Roche		Phase II		Lung, breast, sarcoma, advanced solid tumor
	AMG 4791	Amgen		Phase II	Colon, pancreas, carcinoid, neuroendocrine cell	Lung, ovarian, prostate, sarcoma, advanced solid tumor
	BIIB0221	Biogen Idec		Phase I	Liver	Lung, solid tumor
	MK-0646 (h7C10)2	Merck		Phase II	Colon, pancreas, neuroendocrine cell	Lung, breast, myeloma, advanced solid tumor
	AVE 16422	Sanofi-Aventis		Phase II	Liver	Breast
Tyrosine kinase inhibitors	NVP-AEW5413	Novartis
	NVP-ADW7423	Novartis
	NVP-TAE2263	Novartis	FAK
	BMS-5369243	Bristol Myers Squibb
	BMS-5544173	Bristol Myers Squibb	IR
	BMS-7548073	Bristol Myers Squibb	IR	Phase I/II	Colon	Breast, head and neck, advanced solid tumor
	EGCG (tea polyphenol)3			Phase II	Esophagus	Lung, breast, prostate, bladder, leukemia
	OSI-906 (PQIP)3	OSI pharma		Phase III	Colon, liver	Adrenocortical, ovarian, breast, advanced solid tumor
	A-9286053	Abbott
	XL-228	Exelixis	Abl, SFK, Src, Aurora kinase A	Phase I		CML, lymphoma, cancer
	BVP-51004 (cyclolignan PPP)4	Biovitrum
	INSM-184 [Nordihydroguaiaretic acid (NDGA)]	INSMED	Her2	Phase II		Prostate, brain, advanced solid tumor, leukemia, MDS, lymphoma
Dominant negative mutants	IGF-IR/482st
	IGF-IR/486STOP
	IGF-IR/950st
	IGF-IR/952STOP
Antibodies for the ligands	KM1468	Kyowa Hakko
	KM3168	Kyowa Hakko
	KM3002	Kyowa Hakko
IGFBPs	Recombinant human IGFBP3 protein

¹Fully human antibody;

²Humanized antibody;

³Adenosine triphosphate (ATP) antagonists;

⁴Non-ATP antagonists. IGF-IR: Type I insulin-like growth factor receptor; GI: Gastrointestinal; HCC: Hepatocellular carcinoma; CMPD: Chronic myeloproliferative disorder; FAK: Focal adhesion kinase; CML: Chronic myeloid leukaemia; MDS: Myelodysplastic syndromes; IGFBP: IGF binding protein.