Table 2.

List of neurokinin antagonist in clinical trials.

S.No	Antagonists	NCT No.	Stage of clinical trials	Diseases	Receptor	Functions	References
1	GR205171	NCT003886	Phase 2	Psychiatric disorders	NK1R	Blockage of NK1R	(Kramer et al., 1998), (Mathew et al., 2011; Rupniak et al., 2000)
		NCT006097 NCT013819	Phase 2 Phase 1
2	SB-223412	NCT001027	Phase 2	Psychotic drug (Schizophrenia)	NK3R	Modulate monoaminergic neurotransmission	(Dawson et al., 2008; de la Flor and Dawson, 2009; Sanger, 2004)
	Talnetant	NCT003063	Phase 2
		NCT000446	Phase 2
3	SB-223412	NCT001085	Phase 2	IBS	NK3R	Modulate monoaminergic neurotransmission	Sanger (2004)
	Talnetant
4	SR-142-801 Osanetant			Drug addiction, schizophrenia,	NK3R	Inhibit NKB binding to its receptor; modulate dopaminergic activity in the core of the nucleus accumbens.	(De Souza Silva et al., 2006; Emonds-Alt et al., 1995; Jocham et al., 2006; Quartara and Altamura, 2006)
5	T-2328			Chemotherapy-induced emesis	NK1R	Inhibit the specific binding of SP to its receptor NK1R in the vomiting center	Watanabe et al. (2008)
6	L-773,060			Psychiatric disorders	NK1R	Blockage of NK1R	Kramer et al. (1998)
	L-760,735
7	Fosaprepitat (also known as MK-0517 and L758,298 (FDA approved)	NCT017317	Phase 2	Chemotherapy	NK1R	Inhibit the specific binding of SP to its receptor NK1R in the vomiting center	(Navari, 2008) (Adra et al., 2016; Van Laere et al., 2012; Weinstein et al., 2016, 2018)
		NCT009421	Phase 1	Induced nausea and vomiting
		NCT016979	Phase 2
		NCT015949	Phase3
		NCT008159	Phase 1
		NCT011151	Phase 1
		NCT009921	Phase 1
8	MK-0869	NCT009541	Phase 3	Cisplatin	NK1R	Inhibit the specific binding of SP to its receptor NK1R in the vomiting center, an inhibitor of CYP3A4	(de Wit et al., 2003; Tattersall et al., 2000)
		NCT009921	Phase 1	chemotherapy			Hu et al. (2014)
		NCT000309	Phase 3
		NCT000983	Phase 4
9	MK-0869	NCT000407	Phase 3	Major depressive disorder	NK1R	Inhibit the specific binding of SP to its receptor NK1R	(Keller et al.; Snyder et al., 2018)
		NCT000309	Phase 3
		NCT000383	Phase 3
		NCT000494	Phase 3
		NCT000348	Phase 3
		NCT000429	Phase 3
		NCT000382	Phase 3
		NCT000344	Phase 4
		NCT000395	Phase 3
10	Nepadutant			Asthma, Post-operative ileus	NK2R	Inhibits NKA binding to its receptor; NK2R	(Carini et al., 2001; Quartara et al., 2009)
							Schelfhout et al. (2009)
11	Nepadutant	NCT006583	Phase 1	IBS (Gastrointestinal disorders)	NK2R	Inhibits NKA binding to its receptor; NK2R	(Carini et al., 2001; Quartara et al., 2009)
		NCT015318 NCT012553	Phase 2
			Phase 2
12	Ibodutant	NCT021096	Phase 3	IBS	NK2R	Inhibits NKA binding to its receptor; NK2R	(Quartara et al., 2009; Szymaszkiewicz et al., 2019; Tack et al., 2016)
		NCT013024	Phase 2
13	DNK-333	NCT006966	Phase 2	IBS	NK1R/NK2R	It binds with similar and high affinities to human NK1R and NK2R receptors.	(Joos et al., 2004; Quartara et al., 2009; Zakko et al., 2011)
		NCT003973	Phase 2
	DNK-333			Asthma		Protect against NKA induced bronchoconstriction.	Joos et al. (2004)
	DNK-333	NCT010397	Phase 2	Atopic Dermatitis	NK1R/NK2R	It binds with similar and high affinities to human NK1R and NK2R.	–
14	Rolapitant		Phase 1	Chemotherapy-induced nausea	NK1R	Inhibit the specific binding of SP to its receptor NK1R in the area of postrema, nucleus tractus solitaries, and visceral afferent nerves.	Rapoport et al. (2015)
			Phase 3
		NCT022847	Phase 3
		NCT014949	Phase 3
		NCT015026	Phase 1
		NCT015013	Phase 1
		NCT023866	Phase 2
		NCT024361	Phase 2
		NCT005321
		NCT003966
15	Rolapitant	NCT005321	Phase 2	cough	NK1R	Inhibit the specific binding of SP to its receptor NK1R	–
16	Saredutant	NCT003933	Phase 3	Depressive disorder	NK2R	Potentially block the binding of NKA to its receptor.	Micale et al. (2008)
		NCT003313	Phase 3
		NCT004260	Phase 3
		NCT003950	Phase 3
		NCT002514	Phase 3
		NCT002501	Phase 3
		NCT002553	Phase 3
		NCT004118	Phase 3