Table 1.

WNT-targeted therapeutics

Node	Target	Drug	CRC Model	Efficacy in vivo	Stage	Source
Ligand/Receptor	Porcupine	WNT974	Human CRC organoids, GEMMs	Yes*	Phase 1	[41, 63, 64]
		ETC-159	PDX	Yes	Pre-clinical	[31]
		C59	GEMM	Yes		[65]
	RSPO	OMP-131R10	Xenografts, GEMMs	Yes	Phase 1	[32]#
	FZD receptor	OMP-18R5	PDX	Yes	Phase 1	[61]
		OMP-54F28	Cell lines, PDX	Yes	Phase 1	[85]
	LRP6	GSK3178022	Cell lines, xenograft, PDX	Yes	Pre-clinical	[86]
Destruction Complex	Tankyrase	XAV939	CRC lines	N/A	Pre-clinical	[87]
		JW55	CRC lines	Yes	Pre-clinical	[88]
		NVP-TNKS656	CRC lines, PDX	Yes	Pre-clinical	[69]
		G007-LK	Cell lines, xenografts, GEMMS	Dose-limiting toxicity	Pre-clinical	[89]
		G631	Xenografts	Dose-limiting toxicity	Pre-clinical	[90]
Transcription	β-catenin/TCF	ICG-001 (PRI-724)	CRC lines, xenograft, Human trial	Yes	Phase 1/2	[71]
		2,4-diamino-quinazoline	CRC lines, xenograft	No	Pre-clinical	[91]
		PNU-74654	CRC lines	N/A	Pre-clinical	[92]
		iCRT3, iCRT5, iCRT14	CRC lines, GEMMS	Yes*	Pre-clinical	[72, 74, 75]
		CCT036477	CRC lines, β-catenin mutant mice	No	Pre-clinical	[60]

^#Reference describes an RSPO3 Antibody developed by Genentech, OMP-131R10 has not been published

^*Non-CRC tumors

PDX– Patient-derived xenograft

Xenografts– Refers to CRC lines subcutaneously engrafted into immunocompromised mice