netupitant profile

netupitant: orally active neurokinin-1 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

netupitant : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-[3,5-bis(trifluoromethyl)phenyl]-2-methylpropanoic acid with the secondary amino group of N-methyl-4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-amine; an antiemetic used in combination with palonosetron hydrochloride (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	6451149
CHEMBL ID	206253
CHEBI ID	85155
SCHEMBL ID	445804
MeSH ID	M0496224

Synonym
D05152
290297-26-6
netupitant (usan/inn)
netupitant
cid6451149
ro 67-3189/000
CHEMBL206253 ,
chebi:85155 ,
ro-67-3189
ro-673189000
2-[3,5-bis(trifluoromethyl)phenyl]-n,2-dimethyl-n-[4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-yl]propanamide
2-(3,5-bis(trifluoromethyl)phenyl)-n,2-dimethyl-n-(6-(4-methylpiperazin-1-yl)-4-o-tolylpyridin-3-yl)propanamide
bdbm50178574
2-(3,5-bis(trifluoromethyl)phenyl)-n-methyl-n-(4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-yl)-2-methylpropanamide
netupitant [usan:inn]
benzeneacetamide, n,alpha,alpha-trimethyl-n-(4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl)-3,5-bis(trifluoromethyl)-
unii-7732p08tir
7732p08tir ,
S4654
akynzeo capsule component netupitant
netupitant [usan]
netupitant [vandf]
netupitant [inn]
ro-67-3189/000
netupitant component akynzeo capsule
netupitant [mi]
netupitant [who-dd]
netupitant [orange book]
benzeneacetamide, n,.alpha.,.alpha.-trimethyl-n-(4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl)-3,5-bis(trifluoromethyl)-
gtpl5742
ro 67-31898/000
HY-16346
CS-3337
SCHEMBL445804
2-(3,5-bis(trifluoromethyl)phenyl)-n,2-dimethyl-n-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide
2-(3,5-bis(trifluoromethyl)phenyl)-n,2-dimethyl-n-(6-(4-methylpiperazin-1yl)-4-(o-tolyl)pyridin-3yl)propanamide
2-(3,5-bis-trifluoromethyl-phenyl)-n-methyl-n-[6-(4-methyl-piperazin-1-yl)-4-o-tolyl-pyridin-3-yl]-isobutyramide
ro 67-31898
AC-29232
DTXSID50183271
2-[3,5-bis(trifluoromethyl)phenyl]-n,2-dimethyl-n-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]propanamide
DB09048
FT-0699740
AKOS027251056
2-(3,5-bis(trifluoromethyl)phenyl)-n,2-dimethyl-n-(6-(4-methylpiperazin-1-yl)-4-o-tolylpyridin-3-yl)propanamide, aldrichcpr
mfcd25976831
NCGC00390569-01
EX-A2747
cid-6451149
cid 6451149
AS-10239
BCP08751
Q19598139
A14428
GAW ,
2-[3,5-bis(trifluoromethyl)phenyl]-~{n},2-dimethyl-~{n}-[4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-yl]propanamide
SB18973
HMS3887E19
CCG-270121
benzeneacetamide, n,alpha,alpha-trimethyl-n-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]-3,5-bis(trifluoromethyl)-
GLXC-15009
EN300-24106668
n,alpha,alpha-trimethyl-n-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]-3,5-bis(trifluoromethyl)-benzeneacetamide
Z2037279612

Excerpt	Reference	Relevance
"Netupitant is a novel, selective neurokinin-1 receptor antagonist used for prevention of chemotherapy-induced nausea and vomiting, a distressing side effect of chemotherapy. "	( A dose-finding randomized Phase II study of oral netupitant in combination with palonosetron .75 mg intravenous for the prevention of chemotherapy-induced nausea and vomiting in Japanese patients receiving highly emetogenic chemotherapy. Ikeda, N; Inoue, K; Kagamu, H; Kubota, K; Minato, K; Ohyanagi, F; Osaki, A; Saeki, T; Sakai, H; Tamura, T; Tokuda, Y; Yamada, K, 2019)	2.21
"Netupitant is a new highly selective neurokinin-1 receptor antagonist being studied for the prevention of nausea and vomiting in patients undergoing chemotherapy. "	( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of midazolam, erythromycin, and dexamethasone. Lanzarotti, C; Rossi, G, 2013)	2.23
"Netupitant is a new, selective NK1 receptor antagonist under development for the prevention of chemotherapy-induced nausea and vomiting. "	( Netupitant PET imaging and ADME studies in humans. Calcagnile, S; Giuliano, C; Lanzarotti, C; Mair, S; Nisbet, I; Rossi, G; Spinelli, T; Stevens, L, 2014)	3.29
"Netupitant, is a new NK-1 receptor antagonist with a high binding affinity, a long half-life of 90 hours, is metabolized by CYP3A4, and is an inhibitor of CYP3A4."	( Profile of netupitant/palonosetron (NEPA) fixed dose combination and its potential in the treatment of chemotherapy-induced nausea and vomiting (CINV). Navari, RM, 2015)	1.53
"Netupitant is a potent and selective NK(1) receptor antagonist under development in combination with a fixed dose of palonosetron for the prevention of chemotherapy induced nausea and vomiting. "	( Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects. Pietra, C; Rojas, C; Slusher, BS; Stathis, M, 2012)	2.06

Excerpt	Reference	Relevance
"Netupitant has clinical potential in conditions such as chemotherapy induced nausea and vomiting, in which the blockade of NK(1) receptors has been demonstrated valuable for patients."	( In vitro and in vivo pharmacological characterization of the novel NK₁ receptor selective antagonist Netupitant. Calo', G; Camarda, V; Campi, B; Cantoreggi, S; Molinari, S; Pietra, C; Regoli, D; Rizzi, A, 2012)	1.32

Excerpt	Reference	Relevance
"Netupitant was shown to increase the exposure to dexamethasone in a dose-dependent manner with the mean increase in AUC and C max by 72 and 11 %, respectively, on day 1 and by 138 and 75 %, respectively, on day 4 when co-administered with 300 mg of netupitant."	( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of midazolam, erythromycin, and dexamethasone. Lanzarotti, C; Rossi, G, 2013)	1.51

Excerpt	Reference	Relevance
" Netupitant was well tolerated with most treatment emergent adverse events (AEs) being mild."	( Efficacy and safety of repeated dosing of netupitant, a neurokinin-1 receptor antagonist, in treating overactive bladder. Braticevici, B; Haab, F; Krivoborodov, G; Palmas, M; Pietra, C; Zufferli Russo, M, 2014)	1.58
" Adverse events were comparable across groups with no dose response."	( Efficacy and safety of NEPA, an oral combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting following highly emetogenic chemotherapy: a randomized dose-ranging pivotal study. Alyasova, A; Bondarenko, I; Gralla, RJ; Hesketh, PJ; Lisyanskaya, A; Palmas, M; Rizzi, G; Rossi, G, 2014)	0.65
" Safety was assessed primarily by adverse events (AEs), including cardiac AEs; efficacy by complete response (CR: no emesis, no rescue)."	( A phase III study evaluating the safety and efficacy of NEPA, a fixed-dose combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting over repeated cycles of chemotherapy. Balser, C; Borroni, ME; Bosnjak, SM; Gralla, RJ; Hontsa, A; Jordan, K; Rizzi, G; Rossi, G, 2014)	0.62
" Safety was assessed primarily by treatment-emergent adverse events (AEs) and electrocardiograms."	( Phase III safety study of intravenous NEPA: a novel fixed antiemetic combination of fosnetupitant and palonosetron in patients receiving highly emetogenic chemotherapy. Andric, Z; Gralla, RJ; Karthaus, M; Kowalski, D; Navari, R; Radic, J; Rizzi, G; Roeland, E; Schwartzberg, L; Voisin, D, 2018)	0.7
"Results suggest that oral NEPA is effective and safe in preventing CINV in patients with gynecological cancers treated with cisplatin- or carboplatin-based CT."	( Efficacy and Safety of Oral NEPA (Netupitant/Palonosetron), the First Fixed-Combination Antiemetic, in Patients With Gynecological Cancers Receiving Platinum-Based Chemotherapy. Borroni, ME; Bošnjak, SM; Jordan, K; Rizzi, G; Stamatovic, L, 2018)	0.76
" NEPA was well tolerated with no treatment-related adverse events reported."	( Efficacy and safety of netupitant/palonosetron combination (NEPA) in preventing nausea and vomiting in non-Hodgkin's lymphoma patients undergoing to chemomobilization before autologous stem cell transplantation. Benedetti, F; Bonizzoni, E; Bozzoli, V; Capria, S; Chiusolo, P; Codega, P; Cupelli, L; Cupri, A; De Risi, C; Di Renzo, N; Federico, V; Guarini, A; Matera, R; Mazza, P; Mengarelli, A; Messa, AR; Musso, M; Pastore, D; Perrone, T; Scimè, R; Seripa, D; Specchia, G, 2022)	1.03
" Treatment-related adverse events (AEs) were recorded."	( Real-world multicenter study of the safety and efficacy of netupitant plus palonosetron fixed-dose combination to prevent chemotherapy-induced nausea and vomiting among Malaysian patients receiving moderately or highly emetogenic chemotherapy. Abdul Rahman, MHFB; Abdullah, MM; Ahmad Annuar, MA; Ahmad Badruddin, RBA; Chong, KJ; Lai, CNB; Lam, KS; Lau, KL; Low, JSH; Md Yusof, M; Ng, SC; Nonis, JG; Yap, BK, 2022)	0.96

Excerpt	Reference	Relevance
" Serial blood samples were collected over the course of the two studies and pharmacokinetic parameters were determined for all analytes."	( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of midazolam, erythromycin, and dexamethasone. Lanzarotti, C; Rossi, G, 2013)	0.79
"There were no significant pharmacokinetic interactions between netupitant and palonosetron."	( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Calcagnile, S; Henriksson, A; Kammerer, KP; Lanzarotti, C; Rossi, G; Timmer, W, 2013)	1.03
" The method is simple, rapid, and has been applied successfully to a pharmacokinetic study of netupitant and palonosetron in healthy volunteers."	( Development and validation of a rapid LC-MS/MS method for simultaneous determination of netupitant and palonosetron in human plasma and its application to a pharmacokinetic study. Chen, H; Du, J; Li, H; Li, S; Li, W; Ni, Y; Xu, M; Zhou, Y, 2016)	0.88
" This study evaluated the pharmacokinetic profiles of netupitant and palonosetron."	( Complementary Pharmacokinetic Profiles of Netupitant and Palonosetron Support the Rationale for Their Oral Fixed Combination for the Prevention of Chemotherapy-Induced Nausea and Vomiting. Bernareggi, A; Gilmore, J, 2019)	1.03

Excerpt	Reference	Relevance
" Three studies were designed to evaluate the potential drug-drug interaction of netupitant with palonosetron and of the fixed dose combination of netupitant and palonosetron, NEPA, with an inhibitor (ketoconazole), an inducer (rifampicin) and a substrate (oral contraceptives) of CYP3A4."	( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Calcagnile, S; Henriksson, A; Kammerer, KP; Lanzarotti, C; Rossi, G; Timmer, W, 2013)	1.02
" In study 2, 36 subjects received NEPA alone (day 1) and in combination with ketoconazole or rifampicin."	( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Calcagnile, S; Henriksson, A; Kammerer, KP; Lanzarotti, C; Rossi, G; Timmer, W, 2013)	0.79
" This review evaluates potential drug-drug interactions between NETU or NEPA and CYP3A4 substrates/inducers/inhibitors or P-gp substrates in healthy subjects."	( Drug-drug interaction profile of components of a fixed combination of netupitant and palonosetron: Review of clinical data. Calcagnile, S; Cox, D; Kashef, K; Lanzarotti, C; Natale, JJ; Rossi, G; Spinelli, T, 2016)	0.67

Excerpt	Reference	Relevance
" netupitant and palonosetron have high absolute bioavailability (63%-87% and 97%, respectively)."	( Complementary Pharmacokinetic Profiles of Netupitant and Palonosetron Support the Rationale for Their Oral Fixed Combination for the Prevention of Chemotherapy-Induced Nausea and Vomiting. Bernareggi, A; Gilmore, J, 2019)	1.69
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" The objective of the current work was to determine if palonosetron's ability to inhibit receptor signaling crosstalk would influence netupitant's inhibition of the SP-mediated response when the two drugs are dosed together."	( Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects. Pietra, C; Rojas, C; Slusher, BS; Stathis, M, 2012)	0.82
" Netupitant and palonosetron's benefits include a convenient dosage form, dual-targeted mechanism, and favorable side effect profile, while its main limitations are cost and potential logistical issues surrounding administration."	( The role of netupitant and palonosetron in chemotherapy-induced nausea and vomiting. Abramovitz, RB; Gaertner, KM, 2016)	1.72
" Altogether, these data explain the lack of pharmacokinetic interactions between netupitant and palonosetron at absorption, binding, metabolic, or excretory level, thus highlighting their compatibility as the oral fixed combination NEPA, with administration convenience that may reduce dosing mistakes and increase treatment compliance."	( Complementary Pharmacokinetic Profiles of Netupitant and Palonosetron Support the Rationale for Their Oral Fixed Combination for the Prevention of Chemotherapy-Induced Nausea and Vomiting. Bernareggi, A; Gilmore, J, 2019)	1
" This double-blind, randomized, Phase II study investigated the dose-response of oral netupitant in Japanese patients receiving highly emetogenic chemotherapy."	( A dose-finding randomized Phase II study of oral netupitant in combination with palonosetron .75 mg intravenous for the prevention of chemotherapy-induced nausea and vomiting in Japanese patients receiving highly emetogenic chemotherapy. Ikeda, N; Inoue, K; Kagamu, H; Kubota, K; Minato, K; Ohyanagi, F; Osaki, A; Saeki, T; Sakai, H; Tamura, T; Tokuda, Y; Yamada, K, 2019)	0.99
"No dose-response relationship of netupitant in terms of overall CR rate was observed in this study."	( A dose-finding randomized Phase II study of oral netupitant in combination with palonosetron .75 mg intravenous for the prevention of chemotherapy-induced nausea and vomiting in Japanese patients receiving highly emetogenic chemotherapy. Ikeda, N; Inoue, K; Kagamu, H; Kubota, K; Minato, K; Ohyanagi, F; Osaki, A; Saeki, T; Sakai, H; Tamura, T; Tokuda, Y; Yamada, K, 2019)	1.05
"This multicenter, open-label, phase IIa study evaluated the efficacy of every-other-day dosing of NEPA administered during chemomobilization in patients with relapsed-refractory aggressive non-Hodgkin's lymphoma."	( Efficacy and safety of netupitant/palonosetron combination (NEPA) in preventing nausea and vomiting in non-Hodgkin's lymphoma patients undergoing to chemomobilization before autologous stem cell transplantation. Benedetti, F; Bonizzoni, E; Bozzoli, V; Capria, S; Chiusolo, P; Codega, P; Cupelli, L; Cupri, A; De Risi, C; Di Renzo, N; Federico, V; Guarini, A; Matera, R; Mazza, P; Mengarelli, A; Messa, AR; Musso, M; Pastore, D; Perrone, T; Scimè, R; Seripa, D; Specchia, G, 2022)	1.03

Role	Description
antiemetic	A drug used to prevent nausea or vomiting. An antiemetic may act by a wide range of mechanisms: it might affect the medullary control centres (the vomiting centre and the chemoreceptive trigger zone) or affect the peripheral receptors.
neurokinin-1 receptor antagonist	An antagonist at the neurokinin-1 receptor.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
monocarboxylic acid amide	A carboxamide derived from a monocarboxylic acid.
organofluorine compound	An organofluorine compound is a compound containing at least one carbon-fluorine bond.
aminopyridine	Compounds containing a pyridine skeleton substituted by one or more amine groups.
toluenes	Any member of the class of benzenes that is a substituted benzene in which the substituents include one (and only one) methyl group.
N-alkylpiperazine
N-arylpiperazine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	8.4866	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	16.9330	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	15.0916	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	16.9330	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	16.9330	0.0123	8.9648	39.8107	AID1645842
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	39.8107	0.0096	10.5250	35.4813	AID1479145
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	16.9330	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	16.9330	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Substance-P receptor	Homo sapiens (human)	IC50 (µMol)	0.0010	0.0000	0.0952	6.8130	AID779964
Substance-P receptor	Homo sapiens (human)	Ki	0.0010	0.0000	0.7936	8.7470	AID261640
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
aggressive behavior	Substance-P receptor	Homo sapiens (human)
positive regulation of leukocyte migration	Substance-P receptor	Homo sapiens (human)
angiotensin-mediated drinking behavior	Substance-P receptor	Homo sapiens (human)
inflammatory response	Substance-P receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Substance-P receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Substance-P receptor	Homo sapiens (human)
tachykinin receptor signaling pathway	Substance-P receptor	Homo sapiens (human)
long-term memory	Substance-P receptor	Homo sapiens (human)
associative learning	Substance-P receptor	Homo sapiens (human)
detection of abiotic stimulus	Substance-P receptor	Homo sapiens (human)
response to ozone	Substance-P receptor	Homo sapiens (human)
positive regulation of epithelial cell migration	Substance-P receptor	Homo sapiens (human)
response to auditory stimulus	Substance-P receptor	Homo sapiens (human)
regulation of smooth muscle cell migration	Substance-P receptor	Homo sapiens (human)
positive regulation of synaptic transmission, cholinergic	Substance-P receptor	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Substance-P receptor	Homo sapiens (human)
response to estradiol	Substance-P receptor	Homo sapiens (human)
response to progesterone	Substance-P receptor	Homo sapiens (human)
response to nicotine	Substance-P receptor	Homo sapiens (human)
operant conditioning	Substance-P receptor	Homo sapiens (human)
sperm ejaculation	Substance-P receptor	Homo sapiens (human)
eating behavior	Substance-P receptor	Homo sapiens (human)
positive regulation of vascular permeability	Substance-P receptor	Homo sapiens (human)
response to ethanol	Substance-P receptor	Homo sapiens (human)
positive regulation of action potential	Substance-P receptor	Homo sapiens (human)
positive regulation of blood pressure	Substance-P receptor	Homo sapiens (human)
positive regulation of ossification	Substance-P receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Substance-P receptor	Homo sapiens (human)
positive regulation of hormone secretion	Substance-P receptor	Homo sapiens (human)
behavioral response to pain	Substance-P receptor	Homo sapiens (human)
regulation of smooth muscle cell proliferation	Substance-P receptor	Homo sapiens (human)
positive regulation of lymphocyte proliferation	Substance-P receptor	Homo sapiens (human)
positive regulation of epithelial cell proliferation	Substance-P receptor	Homo sapiens (human)
positive regulation of stress fiber assembly	Substance-P receptor	Homo sapiens (human)
response to electrical stimulus	Substance-P receptor	Homo sapiens (human)
smooth muscle contraction involved in micturition	Substance-P receptor	Homo sapiens (human)
positive regulation of uterine smooth muscle contraction	Substance-P receptor	Homo sapiens (human)
positive regulation of flagellated sperm motility	Substance-P receptor	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
tachykinin receptor activity	Substance-P receptor	Homo sapiens (human)
protein binding	Substance-P receptor	Homo sapiens (human)
substance P receptor activity	Substance-P receptor	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	Substance-P receptor	Homo sapiens (human)
cell surface	Substance-P receptor	Homo sapiens (human)
dendrite	Substance-P receptor	Homo sapiens (human)
sperm flagellum	Substance-P receptor	Homo sapiens (human)
cell body	Substance-P receptor	Homo sapiens (human)
sperm head	Substance-P receptor	Homo sapiens (human)
sperm midpiece	Substance-P receptor	Homo sapiens (human)
plasma membrane	Substance-P receptor	Homo sapiens (human)
sperm midpiece	Substance-P receptor	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID261641	Inhibition of GR-73632 induced foot tapping in gerbil, po	2006	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5	Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
AID779964	Antagonist activity at NK1 receptor (unknown origin)	2013	Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21	Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
AID261640	Displacement of [3H]-labeled substance P from cloned human NK1 receptor expressed in CHO cells	2006	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5	Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346346	Human NK1 receptor (Tachykinin receptors)	2006	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5	Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	2 (2.94)	29.6817
2010's	44 (64.71)	24.3611
2020's	22 (32.35)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	19 (27.94%)	5.53%
Reviews	10 (14.71%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	2 (2.94%)	0.25%
Other	37 (54.41%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.	2.31	1	0	nucleobase analogue; organofluorine compound	antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	7.08	1	0	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.	8.47	1	1	imidazobenzodiazepine; monofluorobenzenes; organochlorine compound	anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative
ondansetron Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.	3.59	1	1	carbazoles
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	2.07	1	0	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
quinuclidines Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group.	12.87	30	9	quinuclidines; saturated organic heterobicyclic parent
erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.	8.47	1	1	cyclic ketone; erythromycin
deoxycytidine [no description available]	2.31	1	0	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
substance p [no description available]	8.02	4	0	peptide	neurokinin-1 receptor agonist; neurotransmitter; vasodilator agent
gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.	2.31	1	0	organofluorine compound; pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic
irinotecan [no description available]	2.31	1	0	carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug
6-chloronicotinic acid [no description available]	2.03	1	0	aromatic carboxylic acid; pyridines
cp 96345 CP 96345: structure given in first source; potent nonpeptide antagonist of the substance P (NK1) receptor; CP 96344 is enantiomer of CP 96345	2.08	1	0
(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine: structure given in first source	2.08	1	0
l 733060 3-((3,5-bis(trifluoromethyl)phenyl)methyloxy)-2-phenylpiperidine: RN given refers to (2S-cis)-isomer; L-733,061 is pharmacologically inactive; structure in first source	2.08	1	0	piperidines
atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.	2.07	1	0
carboplatin [no description available]	9.26	3	1
melphalan Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.	2.72	2	0	L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound	alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent
granisetron Granisetron: A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.. granisetron : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 1-methyl-1H-indazole-3-carboxylic acid with the primary amino group of (3-endo)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine. A selective 5-HT3 receptor antagonist, it is used (generally as the monohydrochloride salt) to manage nausea and vomiting caused by cancer chemotherapy and radiotherapy, and to prevent and treat postoperative nausea and vomiting.	7.25	1	0	aromatic amide; indazoles
cp 99994 3-(2-methoxybenzylamino)-2-phenylpiperidine: selective NK(1) receptor antagonist; CP-100263 is the inactive enantiomer	2.21	1	0
palonosetron Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.. palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.	14.53	49	16	azabicycloalkane; delta-lactam; organic heterotricyclic compound	antiemetic; serotonergic antagonist
vofopitant [no description available]	3.48	1	1
vestipitant [no description available]	2.08	1	0
tapentadol Tapentadol: An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES.	2.6	1	0	alkylbenzene
orvepitant [no description available]	2.08	1	0
mocetinostat mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).	2.1	1	0	aminopyrimidine; benzamides; pyridines; secondary amino compound; secondary carboxamide; substituted aniline	antineoplastic agent; apoptosis inducer; autophagy inducer; cardioprotective agent; EC 3.5.1.98 (histone deacetylase) inhibitor; hepatotoxic agent
casopitant [no description available]	2.08	1	0	piperidines
rolapitant [no description available]	2.11	1	0	azaspiro compound; ether; organofluorine compound; piperidines; pyrrolidin-2-ones	antiemetic; neurokinin-1 receptor antagonist
piperidines Piperidines: A family of hexahydropyridines.	3.93	2	1
levoleucovorin Levoleucovorin: A folate analog consisting of the pharmacologically active isomer of LEUCOVORIN.. (6S)-5-formyltetrahydrofolic acid : The pharmacologically active (6S)-stereoisomer of 5-formyltetrahydrofolic acid.	2.31	1	0	5-formyltetrahydrofolic acid	antineoplastic agent; metabolite
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	2.08	1	0	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor
olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.	7.6	1	0	benzodiazepine; N-arylpiperazine; N-methylpiperazine	antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor
aprepitant Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.	5.07	8	1	(trifluoromethyl)benzenes; cyclic acetal; morpholines; triazoles	antidepressant; antiemetic; neurokinin-1 receptor antagonist; peripheral nervous system drug; substance P receptor antagonist

Condition	Indicated	Relationship Strength	Studies	Trials
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	2.03	1	0
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.25	1	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
2019 Novel Coronavirus Disease [description not available]	0	2.31	1	0
Emesis [description not available]	0	14.02	42	13
Colorectal Cancer [description not available]	0	2.31	1	0
Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.	0	13.73	40	12
Vomiting The forcible expulsion of the contents of the STOMACH through the MOUTH.	0	14.02	42	13
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	0	2.31	1	0
Diffuse Mixed Small and Large Cell Lymphoma [description not available]	0	3.8	1	1
Lymphoma, Non-Hodgkin Any of a group of malignant tumors of lymphoid tissue that differ from HODGKIN DISEASE, being more heterogeneous with respect to malignant cell lineage, clinical course, prognosis, and therapy. The only common feature among these tumors is the absence of giant REED-STERNBERG CELLS, a characteristic of Hodgkin's disease.	0	3.8	1	1
Hematologic Malignancies [description not available]	0	2.41	1	0
Hematologic Neoplasms Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES.	0	2.41	1	0
Breast Cancer [description not available]	0	11.23	3	1
Breast Neoplasms Tumors or cancer of the human BREAST.	0	6.23	3	1
Ache [description not available]	0	2.6	1	0
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	0	2.6	1	0
Adverse Drug Event [description not available]	0	4.94	2	1
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	4.94	2	1
Diabetes Mellitus, Adult-Onset [description not available]	0	2.6	1	0
Morbid Obesity [description not available]	0	4.11	2	1
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	0	2.6	1	0
Obesity, Morbid The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2.	0	4.11	2	1
Cancer of Lung [description not available]	0	3.17	1	0
Lung Neoplasms Tumors or cancer of the LUNG.	0	3.17	1	0
Kahler Disease [description not available]	0	2.72	2	0
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	0	2.72	2	0
Benign Neoplasms [description not available]	0	9.73	9	4
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	1	11.73	9	4
Female Genital Neoplasms [description not available]	0	2.17	1	0
Genital Neoplasms, Female Tumor or cancer of the female reproductive tract (GENITALIA, FEMALE).	0	2.17	1	0
Sarcoma, Epithelioid [description not available]	0	2.21	1	0
Sarcoma A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.	0	2.21	1	0
Emesis, Postoperative [description not available]	0	3.59	1	1
Postoperative Nausea and Vomiting Emesis and queasiness occurring after anesthesia.	1	5.59	1	1
Bladder, Overactive [description not available]	0	3.48	1	1
Urge Incontinence [description not available]	0	3.48	1	1
Urinary Bladder, Overactive Symptom of overactive detrusor muscle of the URINARY BLADDER that contracts with abnormally high frequency and urgency. Overactive bladder is characterized by the frequent feeling of needing to urinate during the day, during the night, or both. URINARY INCONTINENCE may or may not be present.	0	3.48	1	1
Urinary Incontinence, Urge Involuntary discharge of URINE that is associated with an abrupt and strong desire to void. It is usually related to the involuntary contractions of the detrusor muscle of the bladder (detrusor hyperreflexia or detrusor instability).	0	3.48	1	1
Colitis Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.	0	7.1	1	0
Neuroblastoma A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)	0	2.1	1	0
Nociceptive Pain Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.	0	2.51	2	0
Visceral Pain Pain originating from internal organs (VISCERA) associated with autonomic phenomena (PALLOR; SWEATING; NAUSEA; and VOMITING). It often becomes a REFERRED PAIN.	0	2.1	1	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	0	2.07	1	0

netupitant

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Synonyms (64)

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Studies (68)

Market Indicators

Research Demand Index: 57.11

Study Types