Table 2.

NAMPT inhibitors in preclinical studies.

Preclinical Drugs	Type	IC50	In Vivo Treatments
GNE617 GNE618 GNE643 GNE875	Oral competitive	5 nM	20–30 mg/kg orally in mice [131,133]
STF-118804	Competitive	<10 nM	50 mg/kg by subcutaneous injections in mice [135]
Nampt-IN-1/LSN3154567	Competitive	3.1 nM	2 mg/kg in mice, 1–2.5 mg/kg or 5 mg/kg (with NA) in dogs [137]
CB30865 CB300919	Competitive	1–10 nM	0.25 mg/kg by intraperitoneal injection in mice [130]
LB-60-OF61	Competitive	30 nM	In MYC-overexpressing cell lines [138]
GPP78/CAY10618	Competitive	3 nM	10 mg/kg by intraperitoneal injection in mice [139]
Compound 30	Competitive	0.13–25.3 nM	15 mg/kg by intravenous injection [140]
TP201565	Competitive		In several human cell lines [136]
MV78	Competitive	3.1 nM	[141]
trans-3-(pyridin-3-yl) acrylamide- sulfamides	Competitive	0.2–5 nM	In several human cell lines [142]
MPC-9528 MPI0479883	Competitive	0.06 nM	75 mg/kg in mice [134]
A-1293201 A-1307138	Oral Competitive	11–900 nM	7.5, 15 or 30 mg/kg orally in mice [143,144]
MS0-MS31	Competitive	0.9–96 nM	In some human cell lines [145,146]
STF-31	Dual inhibitor of GLUT1 and NAMPT	1 µM	In several human cell lines [147]
Nampt-IN-3	Dual inhibitor of NAMPT and HDAC	31–55 nM	25 mg/kg by intraperitoneal injection in mice [148]
Nampt-IN-5	Dual inhibitor of NAMPT and CYP3A4	0.7–3.9 nM	5–30 mg/kg oral gavage in mice [149]
NAMPT inhibitor-ADC1–4	Drug-linker conjugates for ADC (anti-c-Kit)	0.1 pM– 10 nM	3–10 mg/kg by intraperitoneal injection in mice [150,151]
Water-soluble ruthenium complexes	Pro-drug photoactivated chemotherapy (PACT)		In skin and lung human tumour cell lines [152]
Niraparib/Olaparib +NAMPT inhibitors	Combination with synergistic effect		50 mg/kg orally in mice (PARPi) [153]