Table 2.

Summary of the reported combinations of NAMPT inhibitors with other agents in cancer therapy.

NAMPT Inhibitor	The Combination Agent/Drug	Class	Approval as an Anti-Cancer	Cancer Type	In Vitro Efficacy	In Vivo Efficacy	Ref.
FK866	5-fluorouracil	Antimetabolite	Yes	Gastric cancer	Yes	n/a 1	[71]
FK866	Fludarabine	Antimetabolite	Yes	Leukemia (CLL)	Yes	n/a	[135]
FK866	Etoposide	Topoisomerase II inhibitor	Yes	Leukemia	Yes	n/a	[136,137]
GMX1777	Etoposide	Topoisomerase II inhibitor	Yes	Lung cancer	n/a	Yes	[108]
FK866	Etoposide	Topoisomerase II inhibitor	Yes	Neuroblastoma	Yes	n/a	[138]
FK866	Cisplatin	Alkylating agent	Yes	Neuroblastoma	Yes	n/a	[138]
FK866 GMX1778	Cisplatin	Alkylating agent	Yes	Ovarian cancer	Yes	Yes (FK866)	[139]
FK866	Cyclosporin A Verapamil	Pgp inhibitor Pgp inhibitor	No No	Leukemia Leukemia	Yes Yes	n/a n/a	[140]
FK866	Bortezomib	Proteasome inhibitor	Yes	Multiple myeloma	Yes	Yes	[141]
FK866	Ibrutinib	Bruton’s tyrosine kinase inhibitor	Yes	Waldenstrom macroglobulinemia	Yes	Yes	[142]
GMX1777	Pemetrexed	Antimetabolite (Antifolate)	Yes	Non-small-cell lung cancer (NSCLC)	Yes	Yes	[143]
FK866	Gemcitabine	Antimetabolite	Yes	Pancreatic cancer (PDAC)	Yes	n/a	[144]
FK866	Gemcitabine	Antimetabolite	Yes	PDAC	Yes	Yes	[50]
STF-118804	Gemcitabine	Antimetabolite Topoisomerase II inhibitor Antimicrotubular agent	Yes	PDAC	Yes	n/a	[145]
	Etoposide		Yes	PDAC	Yes	n/a
	Paclitaxel		Yes	PDAC	Yes	n/a
FK866	Vorinostat Valproic acid	HDAC inhibitor HDAC inhibitor	Yes No	Leukemia Leukemia	Yes Yes	n/a n/a	[146]
GMX1778	177Lu-DOTATATE	Radiolabeled somatostatin analog	Yes	Neuroendocrine tumors	n/a	Yes	[147]
FK866	Rituximab	Anti-CD20	Yes	Lymphoma	Yes	Yes	[148]
FK866 GMX1778	Temozolomide	Alkylating agent	Yes	Glioblastoma	Yes	n/a	[149]
FK866 GMX1778	Temozolomide	Alkylating agent	Yes	IDH1-mutant cancers	Yes	Yes (FK866)	[150]
FK866	Olaparib	PARP inhibitor	Yes	Triple-negative breast cancer (TNBC)	Yes	Yes	[151]
GNE-618 FK866 GMX1778	Niraparib	PARP inhibitor	Yes	Ewing sarcoma	Yes	Yes (GNE-618)	[152]
OT-82	Niraparib	PARP Inhibitor	Yes	Ewing sarcoma	Yes	Yes	[153]
OT-82	Irinotecan & its metabolite SN-38	topoisomerase I inhibitors	Yes (Irinotecan)	Ewing sarcoma	Yes (SN-38)	Yes (Irinotecan)	[153]
OT-82	Cytarabine	Antimetabolite	Yes	Acute lymphoblastic leukemia (ALL)	Yes	Yes	[154]
OT-82	Dasatinib	Tyrosine kinase inhibitor	Yes	ALL	n/a	Yes	[154]
OT-82	Etoposide	Topoisomerase II inhibitor	Yes	ALL	Yes	n/a	[154]
GMX1778	Anti-mouse PD-1 antibody	Immune checkpoint inhibitor	Human anti-PD1: Yes	Glioblastoma	n/a	Yes	[155]
MV87	Anti-mouse PD-1 antibody	Immune checkpoint inhibitor	Human anti-PD1: Yes	Fibrosarcoma	n/a	Yes	[156]
KPT-9274	Anti-mouse PD-1 antibody	Immune checkpoint inhibitor	Human anti-PD1: Yes	Renal cell carcinoma	n/a	Yes	[157]
KPT-9274	Anti-mouse PD-1 antibody	Immune checkpoint inhibitor	Human anti-PD1: Yes	Melanoma Colon adenocarcinoma	n/a	Yes (PAK4)	[158]
KPT-9274	Bendamustine Melphalan	Alkylating agent Alkylating agent	Yes Yes	Waldenstrom macroglobulinemia	Yes Yes	Yes n/a	[159]
KPT-9274	Everolimus	mTOR inhibitor	Yes	Pancreatic neuroendocrine tumor	Yes	n/a	[160]
KPT-9274	Gemcitabine Oxaliplatin	Antimetabolite Alkylating agent	Yes Yes	PDAC PDAC	Yes Yes	Yes (PAK4) n/a	[161]
FK866	TRAIL	Apoptosis activator	Not approved as a drug	Leukemia	Yes	n/a	[162]
FK866	2-HNA	NAPRT inhibitor	Not approved as a drug	Ovarian cancer Pancreatic cancer	Yes	Yes (sodium salt of 2-HNA)	[62]
FK866	L-1-methyl-tryptophan	Indoleamine 2,3-dioxygenase (IDO) inhibitor	Not approved as a drug	Gastric cancer Bladder cancer	n/a	Yes (only in immuno-competent mice)	[163]
FK866	β-Lapachone	ROS generator & NQO1 substrate	Not approved as a drug	PDAC NSCLC	Yes	n/a	[164,165,166]
FK866	FX11	Lactate dehydrogenase A (LDHA) inhibitor	Not approved as a drug	Lymphoma	Yes	Yes	[167]
FK866	1-methyl-3-nitro-1-nitrosoguanidinium (MNNG)	Alkylating agent	Not approved as a drug	Leukemia	Yes	n/a	[168]

¹ n/a: not available (i.e., not reported in the referred article).