dextromethorphan profile

Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough. [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	5360696
CHEMBL ID	52440
CHEBI ID	4470
CHEBI ID	92579
SCHEMBL ID	29949
MeSH ID	M0006138

Synonym
BRD-K33211335-337-03-7
(+)-3-methoxy-n-methylmorphinan
dextromethorphane
dextrometorfano
destrometerfano
ba 2666
benylin dm
balminil dm
(4as,10s,10as)-6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2h-10,4a-(epiminoethano)phenanthrene
dextromethorphanum
ba-2666
dextromethorfan
CHEBI:4470 ,
(9alpha,13alpha,14alpha)-3-methoxy-17-methylmorphinan
d-methorphan
calmylin
albutussin
3-methoxy-17-methyl-9alpha,13alpha,14alpha-morphinan
dextromorphan
romilar
dxm ,
(9alpha,13alpha,14alpha)-17-methyl-3-(methyloxy)morphinan
dextromethorphan (usp)
D03742
dextromethorfan [czech]
dextromethorphane [inn-french]
morphinan, 3-methoxy-17-methyl-, (9-alpha,13-alpha,14-alpha)-
dextrometorfano [inn-spanish]
einecs 204-752-2
destrometerfano [dcit]
dextromethorphan [usp:inn:ban]
brn 0088549
dextromethorphanum [inn-latin]
9alpha,13alpha,14alpha-morphinan, 3-methoxy-17-methyl-
9-alpha,13-alpha,14-alpha-morphinan, 3-methoxy-17-methyl-
morphinan, 3-methoxy-17-methyl-, (9.alpha.,13.alpha.,14.alpha.)-
NCGC00015333-01
lopac-d-2531
BSPBIO_000457
PRESTWICK2_000359
BPBIO1_000503
( )-3-methoxy-n-methylmorphinon
morphinan, 3-methoxy-17-methyl-, (9alpha,13alpha,14alpha)-
(+)-3-methoxy-17-methylmorphinan
( )-cis-1,3,4,9,10,10a-hexahydro-6-methoxy-11-methyl-2h-10,4alpha-iminoethanophenanthren
9alpha,13alpha,14alpha-morphinan, 3-methoxy-17-methyl- (8ci)
hsdb 3056
delta-methorphan
C06947
dextromethorphan
125-71-3
(+)-dextromethorphan
DB00514
SPBIO_002378
PRESTWICK0_000359
PRESTWICK1_000359
PRESTWICK3_000359
NCGC00015333-02
HMS2090C08
nsc-751452
CHEMBL52440
dextrometorphan
nsc 751452
(+)-3-methoxy-n-methylmorphinon
unii-7355x3rots
4-21-00-01367 (beilstein handbook reference)
dxm [antitussive]
(+)-cis-1,3,4,9,10,10a-hexahydro-6-methoxy-11-methyl-2h-10,4alpha-iminoethanophenanthren
7355x3rots ,
bdbm50366613
nodex
dextromethorphan [hsdb]
dextromethorphan [who-dd]
dextromethorphan [vandf]
dextromethorphan [inn]
dextromethorphan [mart.]
dextromethorphan [usp monograph]
dextromethorphan [usp-rs]
dextromethorphan [mi]
gtpl6953
AKOS025311415
SCHEMBL29949
3-methoxy-17-methyl-9.alpha.,13.alpha.,14.alpha.-morphinan
romilar (salt/mix)
tusilan (salt/mix)
9.alpha.,13.alpha.,14.alpha.-morphinan, 3-methoxy-17-methyl-
3-methoxy-17-methylmorphinan-, (9.alpha.,13.alpha.,14.alpha.)- #
3-methoxy-17-methyl-9.alpha.,13.alpha.-morphinan
racemethorphan [as d-form]
delsym (salt/mix)
medicon (salt/mix)
DTXSID3022908 ,
(1r,9r,10r)-4-methoxy-17-methyl-17-azatetracyclo[7.5.3.0^{1,10}.0^{2,7}]heptadeca-2,4,6-triene
(+)-3-methoxy-17-methyl-9alpha,13alpha,14alpha-morphinan
(1s,9s,10s)-4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-triene
J-005274
3-methoxy-17-methyl-9a,13a,14a-morphinan
(9a,13a,14a)-3-methoxy-17-methylmorphinan
lsm-2726
CHEBI:92579
4-methoxy-12-methyl-12-azatetracyclo[9.3^1.10^.0^2.7^] heptadeca-2(7),3,5-triene
Q407781
morphinan, 3-methoxy-17-methyl-, (9?,13?,14?)-
robotablets
soothe comfort ii cough syrupherbal mint
dextromethorphan (usp monograph)
dextromethorphan (usp:inn:ban)
dextrometorfano (inn-spanish)
dxm (antitussive)
dextromethorphane (inn-french)
dtxcid202908
soothe comfort i cough syruporiginal
dextromethorphan (usp-rs)
dextromethorphan (mart.)
dextromethorphanum (inn-latin)
dextromethorphanum (latin)
delsym (dextromethorphan)
dextromethorphan, 1mg/ml in methanol

Excerpt	Reference	Relevance
"Dextromethorphan polistirex is an extended-release formulation of dextromethorphan hydrobromide, marketed as Delsym® (Reckitt; Parsippany, NJ), with a duration of action roughly two to three times that of the standard formulation. "	( Life-threatening pediatric dextromethorphan polistirex overdose. Foreman, E; Friedland, S; Lasoff, DR; McDaniel, MA; Raviendran, R; Seltzer, JA; Sheth, SK; Toney, C, 2022)	2.46
"Dextromethorphan is an over-the-counter antitussive drug, whereas levomethorphan is strictly controlled as a narcotic drug."	( Chiral analysis of dextromethorphan and levomethorphan in human hair by liquid chromatography-tandem mass spectrometry. Ji, JJ; Shen, M; Xiang, P; Yan, H; Zhao, J, 2022)	1.77
"Dextromethorphan (DXM) is an effective over-the-counter antitussive with an alarming increase as an abused drug for recreational purposes. "	( Targeting mediodorsal thalamic CB1 receptors to inhibit dextromethorphan-induced anxiety/exploratory-related behaviors in rats: The post-weaning effect of exercise and enriched environment on adulthood anxiety. Alijanpour, S; Banaei-Boroujeni, G; Nazari-Serenjeh, F; Rezayof, A, 2023)	2.6
"Dextromethorphan (DXM) is a safe and effective antitussive agent present in several over the counter cough and cold medications. "	( Pharmacokinetics and pharmacodynamics of dextromethorphan: clinical and forensic aspects. Dinis-Oliveira, RJ; Silva, AR, 2020)	2.27
"Dextromethorphan is a noncompetitive N-methyl-d-aspartate (NMDA) receptor antagonist that has produced antidepressant-like effects in forced swim and tail suspension tests (TST); however, the rapid and sustained antidepressant-like effects of dextromethorphan have not been evaluated."	( Assessment of the rapid and sustained antidepressant-like effects of dextromethorphan in mice. Garrett, PI; Hillhouse, TM; Honeycutt, SC; Peterson, AM; Saavedra, JS; White, JW, 2020)	1.51
"Dextromethorphan acts as an antagonist at the glutamate N-methyl-d-aspartate (NMDA) receptor, in addition to other pharmacodynamics properties that include activity at sigma-1 receptors."	( Dextromethorphan/quinidine pharmacotherapy in patients with treatment resistant depression: A proof of concept clinical trial. Ahle, G; Charney, DS; Collins, KA; Iosifescu, DV; Kiraly, DD; Murrough, JW; Sayed, S; Soleimani, L; Wade, E; Welch, A, 2017)	2.62
"Dextromethorphan (DM) is a dextrorotatory isomer of levorphanol, a typical morphine-like opioid. "	( MK-801, but not naloxone, attenuates high-dose dextromethorphan-induced convulsive behavior: Possible involvement of the GluN2B receptor. Chung, YH; Jang, CG; Jeong, JH; Kim, HC; Nabeshima, T; Nah, SY; Shin, EJ; Tran, HQ; Tran, TV; Yamada, K, 2017)	2.15
"Dextromethorphan is a potent noncompetitive antagonist of the NMDA receptor channel that is safe for use in young girls with Rett syndrome. "	( Randomized open-label trial of dextromethorphan in Rett syndrome. Bibat, G; Brereton, N; Ewen, JB; Gupta, S; Hong, M; Johnston, MV; Kelley, R; Kratz, L; Naidu, S; Sanyal, A; Smith-Hicks, CL; Tierney, E; Vaurio, R; Yenokyan, G, 2017)	2.18
"Dextromethorphan is a centrally acting antitussive drug, while its enantiomer levomethorphan is an illicit drug with opioid analgesic effects. "	( Development of a capillary electrophoresis method for the determination of the chiral purity of dextromethorphan by a dual selector system using quality by design methodology. Heuermann, M; Krait, S; Scriba, GKE, 2018)	2.14
"Dextromethorphan is an antitussive with a high margin of safety that has been hypothesized to display rapid-acting antidepressant activity based on pharmacodynamic similarities to the N-methyl-D-aspartate (NMDA) receptor antagonist ketamine. "	( Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan. Healy, JR; Matsumoto, RR; Nguyen, L; Robson, MJ; Scandinaro, AL, 2014)	2.08
"Dextromethorphan is an over-the-counter antitussive agent that may be a rapidly acting treatment for bipolar depression. "	( The utility of the combination of dextromethorphan and quinidine in the treatment of bipolar II and bipolar NOS. Kelly, TF; Lieberman, DZ, 2014)	2.12
"Dextromethorphan (DXM) is a derivative of codeine with an antitussive properties. "	( [Age and gender trends of inpatient recreational acute dextromethorphan intoxication hospitalized in Pomeranian Center of Toxicology between 2009-2011]. Schetz, D; Sein Anand, J; Zając, M, 2014)	2.09
"Dextromethorphan (DM) is an antitussive with rapid acting antidepressant potential based on pharmacodynamic similarities to ketamine. "	( Involvement of AMPA receptors in the antidepressant-like effects of dextromethorphan in mice. Matsumoto, RR; Nguyen, L, 2015)	2.1
"Dextromethorphan (DXM) is a widely available antitussive that has, at elevated dose levels, euphoric and dissociative effects. "	( Patterns and Perceptions of Dextromethorphan Use in Adult Members of an Online Dextromethorphan Community. Gabriel, KI; McDonald, MP; Pringle, G, )	1.87
"Dextromethorphan (DM) is a commonly used antitussive and is currently the only FDA-approved pharmaceutical treatment for pseudobulbar affect. "	( Dextromethorphan: An update on its utility for neurological and neuropsychiatric disorders. Cavendish, JZ; Crowe, MS; Lucke-Wold, BP; Matsumoto, RR; Nguyen, L; Thomas, KL, 2016)	3.32
"Dextromethorphan (DM) is a non-competitive antagonist of NMDA receptors and a widely used component of cough medicine. "	( Prevention of Hippocampal Neuronal Damage and Cognitive Function Deficits in Vascular Dementia by Dextromethorphan. Deng, J; Lu, K; Xu, X; Zhang, B; Zhao, BQ; Zhao, F; Zhao, Y, 2016)	2.09
"Dextromethorphan (DXM) is an antitussive drug found in commonly used nonprescription cold and cough medications. "	( Determination of Dextromethorphan in Oral Fluid by LC-MS-MS. Amaratunga, P; Clothier, M; Lemberg, D; Lorenz Lemberg, B, 2016)	2.22
"Dextromethorphan is a safe, effective cough suppressant, available without a prescription in the United States since 1958. "	( Dextromethorphan: a case study on addressing abuse of a safe and effective drug. Loyd, CM; Skor, EE; Spangler, DC, 2016)	3.32
"Dextromethorphan is a cough suppressant agent with potential antidepressant activity reported in mouse force swimming test."	( The role of NMDA receptor and nitric oxide/cyclic guanosine monophosphate pathway in the antidepressant-like effect of dextromethorphan in mice forced swimming test and tail suspension test. Akbarian, R; Chamanara, M; Dehpour, AR; Khan, MI; Norouzi-Javidan, A; Ostadhadi, S; Sakhaee, E; Yousefi, F; Zolfaghari, S, 2017)	1.38
"Dextromethorphan (DM) is a widely used antitussive reported to exert anti-inflammatory effect in vivo."	( Effects of dextromethorphan on MDMA-induced serotonergic aberration in the brains of non-human primates using [ Chang, KW; Chen, CF; Cheng, CY; Chueh, SH; Hsu, TH; Huang, WS; Huang, YS; Liao, MH; Liu, TT; Ma, KH; Sung, CC; Weng, SJ, 2016)	1.55
"Dextromethorphan is a widely available over-the-counter antitussive that produces intoxicating, hallucinogenic, and dissociative effects at doses significantly exceeding the therapeutic range. "	( Five deaths resulting from abuse of dextromethorphan sold over the internet. Goldfogel, G; Hamilton, R; Kuhlman, J; Logan, BK, 2009)	2.07
"Dextromethorphan is a nonprescription antitussive which has been gaining in popularity as an abused drug, because of the hallucinogenic, dissociative, and intoxicating effects it produces at high doses. "	( Combined dextromethorphan and chlorpheniramine intoxication in impaired drivers. Logan, BK, 2009)	2.21
"Dextromethorphan is a psychotropic substance that carries a potential for abuse and dependence. "	( Dextromethorphan withdrawal and dependence syndrome. Grosshans, M; Hermann, D; Kiefer, F; Koopmann, A; Mann, K; Mutschler, J, 2010)	3.25
"Dextromethorphan (DEX) is a widely used non-opioid antitussive. "	( Dextromethorphan inhibits the glutamatergic synaptic transmission in the nucleus tractus solitarius of guinea pigs. Haji, A; Ohi, Y; Tsunekawa, S, 2011)	3.25
"Dextromethorphan (DEX) is an antitussive agent used in many cough and cold medications, and dextrorphan (DOR) is its metabolite. "	( Simultaneous determination of dextromethorphan and its metabolite dextrorphan in plasma samples using second-order calibration coupled with excitation-emission matrix fluorescence. Liu, YJ; Nie, JF; Ouyang, LQ; Wang, JY; Wu, HL; Yu, RQ, 2011)	2.1
"Dextromethorphan (DM) is a dextrorotary morphinan and a widely used component of cough medicine. "	( Low dose dextromethorphan attenuates moderate experimental autoimmune encephalomyelitis by inhibiting NOX2 and reducing peripheral immune cells infiltration in the spinal cord. Chechneva, OV; Daugherty, DJ; Deng, W; Hong, JS; Mayrhofer, F; Pleasure, DE, 2011)	2.23
"Dextromethorphan is a low-affinity N-methyl-D-aspartate receptor inhibitor."	( Comparative effects of triflusal, S-adenosylmethionine, and dextromethorphan over intestinal ischemia/reperfusion injury. Alarcón-Galván, G; Cámara-Lemarroy, CR; Cordero-Pérez, P; Fernández-Garza, NE; Guzmán-de la Garza, FJ; Muñoz-Espinosa, LE; Torres-Gonzalez, L, 2011)	1.33
"Dextromethorphan (DM) is a well-known probe drug for CYP2D6 and metabolic ratio (MR) is often used to measure the enzyme activity in vivo."	( Inter-individual variability of in vivo CYP2D6 activity in different genotypes. Chiba, K; Ito, T; Kato, M; Sugiyama, Y; Suwa, T, 2012)	1.1
"Dextromethorphan (DM) is a well-known antitussive dextrorotatory morphinan. "	( Dextromethorphan-induced psychotoxic behaviors cause sexual dysfunction in male mice via stimulation of σ-1 receptors. Bach, JH; Chung, YH; Jeong, JH; Kim, HC; Kim, KW; Kwon, YB; Li, Z; Nabeshima, T; Nam, Y; Park, ES; Shin, EJ; Yang, BK, 2012)	3.26
"Dextromethorphan (DM) is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist that may be neuroprotective for monoamine neurons. "	( The DRD2/ANKK1 gene is associated with response to add-on dextromethorphan treatment in bipolar disorder. Chang, YH; Chen, SH; Chen, SL; Chu, CH; Huang, SY; Lee, IH; Lee, SY; Lu, RB; Tzeng, NS; Wang, CL; Yang, YK; Yeh, TL, 2012)	2.07
"Dextromethorphan is a commonly encountered antitussive medication which has found additional therapeutic use in the treatment of pseudobulbar disorder and as an adjunct to opiate use in pain management. "	( Dextromethorphan abuse leading to assault, suicide, or homicide. Frost, MP; Goldfogel, G; Logan, BK; Sandstrom, G; Wickham, DJ; Yeakel, JK, 2012)	3.26
"Dextromethorphan is a noncompetitive NMDA-receptor antagonist."	( Dextromethorphan for phantom pain attenuation in cancer amputees: a double-blind crossover trial involving three patients. Ben Abraham, R; Kollender, Y; Marouani, N; Meller, I; Weinbroum, AA, )	2.3
"Dextromethorphan is a widely used anti-tussive drug with non-competitive antagonistic effects on excitatory amino acid receptors of the N-methyl-D-aspartate (NMDA) type. "	( Dextromethorphan alters gene expression in rat brain hippocampus and cortex. Ahn, JI; Kim, SH; Koh, HC; Lee, KH; Lee, YS; Yang, BH; Yu, DH, 2003)	3.2
"Dextromethorphan is an N-methyl-D-aspartic acid antagonist which can attenuate acute pain with few side-effects. "	( Dextromethorphan and intrathecal morphine for analgesia after Caesarean section under spinal anaesthesia. Choi, DM; Douglas, MJ; Kliffer, AP, 2003)	3.2
"Dextromethorphan is an effective and safe antitussive, but has liabilities with respect to its abuse potential at doses above the therapeutic dose. "	( Determination of dextromethorphan and its metabolites in rat serum by liquid-liquid extraction and liquid chromatography with fluorescence detection. Gurley, BJ; Hendrickson, HP; Wessinger, WD, 2003)	2.1
"Dextromethorphan is a weak noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist. "	( Comparison of the effects of dextromethorphan, dextrorphan, and levorphanol on the hypothalamo-pituitary-adrenal axis. Pechnick, RN; Poland, RE, 2004)	2.06
"Dextromethorphan is an N-methyl-D-aspartate (NMDA) noncompetitive antagonist which has been used as an antitussive, analgesic adjunct, probe drug, experimentally to attenuate acute opiate and ethanol withdrawal, and as an anticonvulsant. "	( Plasma profile and pharmacokinetics of dextromethorphan after intravenous and oral administration in healthy dogs. Kukanich, B; Papich, MG, 2004)	2.04
"Dextromethorphan is an over-the-counter dissociative agent of increasing popularity as a drug of abuse among younger adolescents. "	( Dextromethorphan abuse. Boyer, EW, 2004)	3.21
"Dextromethorphan (DM) is a dextrorotatory morphinan and an over-the-counter non-opioid cough suppressant. "	( Protective effect of dextromethorphan against endotoxic shock in mice. Block, ML; Cui, G; Hong, JS; Li, G; Liu, B; Liu, J; Liu, Y; Qin, L; Tzeng, NS; Wang, T; Wilson, B, 2005)	2.09
"Dextromethorphan is a commonly used antitussive agent that can be purchased over the counter. "	( Dextromethorphan-induced delirium and possible methadone interaction. Lotrich, FE; Pollock, BG; Rosen, J, 2005)	3.21
"Dextromethorphan is an opiod-derived, easily available cough remedy that, when used in large quantities, can have stimulatory effects which mimic that of amphetamine and other psychedelic drugs. "	( Dextromethorphan abuse in Thai adolescents: A report of two cases and review of literature. Chomchai, C; Manaboriboon, B, 2005)	3.21
"Dextromethorphan (DXM) is a cough-suppressing ingredient in a variety of over-the-counter cough and cold medications. "	( Effects of dextromethorphan on in vitro contractile responses of mouse and rat urinary bladders. Levin, RM; Millington, WR; Sourial, MW; Tadrous, M; Whitbeck, C, 2006)	2.17
"Dextromethorphan (DM) is a noncompetitive N-methyl-d-aspartate (NMDA) receptor antagonist, which is widely used as an antitussive agent. "	( Dextromethorphan: a review of N-methyl-d-aspartate receptor antagonist in the management of pain. Drachtman, R; Siu, A, 2007)	3.23
"Dextromethorphan (DXM) is a common component of combination cold medications that has become a popular drug of abuse for young adults. "	( "Crystal dex:" free-base dextromethorphan. Cloutier, RL; Hendrickson, RG, 2007)	2.09
"Dextromethorphan is a synthetic analogue of codeine used in hundreds of over-the-counter medications for its antitussive effects. "	( Dextromethorphan in Wisconsin drivers. Cochems, A; Harding, P; Liddicoat, L, 2007)	3.23
"Dextromethorphan is a widely used antitussive agent, also showing increased recreational abuse. "	( Oral administration of dextromethorphan does not produce neuronal vacuolation in the rat brain. Carliss, RD; Chengelis, CP; O'Neill, TP; Radovsky, A; Shuey, DL, 2007)	2.09
"Dextromethorphan (DXM) is a common ingredient in several prescriptions and over-the-counter cough preparations. "	( Dextromethorphan-induced near-fatal suicide attempt in a slow metabolizer at cytochrome P450 2D6. Kennedy, CA; Kurani, A; Liu, QY; Matin, N, 2007)	3.23
"Dextromethorphan (DM) is a widely-used antitussive. "	( Dextromethorphan as a potential neuroprotective agent with unique mechanisms of action. Calef, U; Lauterbach, EC; Werling, LL, 2007)	3.23
"Dextromethorphan (DEM) is a widely used probe drug for human cytochrome P450 2D6 isozyme activity assessment by measuring the ratio between DEM and its N-demethylated metabolite dextrorphan (DOR). "	( Development and validation of a chemical hydrolysis method for dextromethorphan and dextrophan determination in urine samples: application to the assessment of CYP2D6 activity in fibromyalgia patients. Cherkaoui, S; Daali, Y; Dayer, P; Desmeules, JA; Doffey-Lazeyras, F, 2008)	2.03
"Dextromethorphan (DMP) is an effective and widely used antitussive drug. "	( An evaluation of the genotoxicity of the antitussive drug Dextromethorphan. Aardema, MJ; Gatehouse, D; Johnston, G; Robison, SH, 2008)	2.03
"Dextromethorphan (DM) is a low-affinity, non-competitive NMDA receptor antagonist that has shown promise in preclinical and preliminary clinical studies for the reduction of opioid withdrawal symptoms, but when used at higher doses, it is associated with deleterious side effects attributed to its metabolite, dextrorphan. "	( Dextromethorphan and quinidine combination for heroin detoxification. Akerele, E; Bisaga, A; Comer, SD; Garawi, F; Kleber, HD; Nunes, EV; Sullivan, MA; Thomas, AA, )	3.02
"Dextromethorphan is a dextrorotary morphinan without affinity for opioid receptors, commonly used as an antitussive medication. "	( Dextromethorphan: cellular effects reducing neuronal hyperactivity. Netzer, R; Trube, G, 1994)	3.17
"1. Dextromethorphan is a widely used antitussive agent which is a non-narcotic codeine analogue. "	( The effect of inhaled and oral dextromethorphan on citric acid induced cough in man. Grattan, TJ; Higgins, KS; Marshall, AE; Morice, AH, 1995)	1.2
"Dextromethorphan is a weak noncompetitive N-methyl-D-aspartate (NMDA) antagonist and higher doses or other potent NMDA receptor antagonists should be tested."	( A controlled one-year trial of dextromethorphan in amyotrophic lateral sclerosis. Azulay, JP; Besse, D; Billé-Turc, F; Blin, O; Braguer, D; Branger, E; Crevat, A; Desnuelle, C; Pouget, JY; Serratrice, G, 1996)	1.3
"Dextromethorphan is a widely used antitussive agent with non-competitive antagonistic effects at the excitatory amino acid receptors of the NMDA type. "	( Dextromethorphan reduces intravenous cocaine self-administration in the rat. Balducci, C; Koob, GF; Pulvirenti, L, 1997)	3.18
"Dextromethorphan is a NMDA-glutamate receptor antagonist with neuroprotective properties."	( A clinical trial of dextromethorphan in amyotrophic lateral sclerosis. Bak, S; Boysen, G; Christensen, PB; Gredal, O; Hinge, HH; Jensen, TS; Jespersen, JH; Kristensen, MO; Regeur, L; Werdelin, L, 1997)	1.34
"Dextromethorphan is a noncompetitive antagonist of this receptor with a favorable safety profile."	( The effect of the N-methyl-D-aspartate receptor antagonist dextromethorphan on perioperative brain injury in children undergoing cardiac surgery with cardiopulmonary bypass: results of a pilot study. Arbenz, U; Bandtlow, C; Bauersfeld, U; Baumann, P; Boltshauser, E; Fanconi, S; Huisman, TA; Martin, E; Molinari, L; Schmid, ER; Schmitt, B; Superti-Furga, A; Turina, M; Wohlrab, G, 1997)	1.26
"Dextromethorphan is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist known to inhibit wind-up and central hyperexcitability of dorsal horn neurones. "	( Effect of systemic N-methyl-D-aspartate receptor antagonist (dextromethorphan) on primary and secondary hyperalgesia in humans. Brennum, J; Dahl, JB; Dirks, J; Ilkjaer, S; Wernberg, M, 1997)	1.98
"Dextromethorphan is a nonopioid antitussive metabolized by cytochrome P450 2D6 (CYP2D6) to an active metabolite, dextrorphan. "	( Psychotropic effects of dextromethorphan are altered by the CYP2D6 polymorphism: a pilot study. Busto, UE; Kaplan, HL; Sellers, EM; Tyndale, RF; Zawertailo, LA, 1998)	2.05
"Dextromethorphan is an N-methyl-D-aspartate (NMDA) receptor antagonist which has been shown to inhibit the development of cutaneous secondary hyperalgesia after tissue trauma. "	( Dextromethorphan and pain after total abdominal hysterectomy. Campbell, WI; McCaughey, W; McConaghy, PM; McSorley, P, 1998)	3.19
"Dextromethorphan 1 is an effective neuroprotectant in animal models of epilepsy and ischemia but showed side-effects during clinical trials limiting its potential use in a clinical setting. "	( Synthesis and preliminary biological evaluation of new alpha-amino amide anticonvulsants incorporating a dextromethorphan moiety. Bonsignori, A; Caccia, C; Maj, R; McArthur, RA; Pevarello, P; Salvati, P; Traquandi, G; Varasi, M, 1999)	1.96
"Dextromethorphan is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist known to inhibit wind-up and NMDA-mediated nociceptive responses of dorsal horn neurons. "	( Effect of preoperative oral dextromethorphan on immediate and late postoperative pain and hyperalgesia after total abdominal hysterectomy. Bach, LF; Dahl, JB; Ilkjaer, S; Nielsen, PA; Wernberg, M, 2000)	2.04
"Dextromethorphan is a weak N-methyl-d-aspartate (NMDA) receptor antagonist that inhibits spinal cord sensitization in animal models of pain and also inhibits the development of cutaneous secondary hyperalgesia after tissue trauma. "	( Large-dose oral dextromethorphan as an adjunct to patient-controlled analgesia with morphine after knee surgery. Clarke, D; Goodchild, CS; Wadhwa, A; Young, D, 2001)	2.1
"Dextromethorphan syrup is a safe, non-narcotic medication that significantly reduced the requirement of intravenous morphine after pediatric adenotonsillectomy. "	( Improved postoperative pain control in pediatric adenotonsillectomy with dextromethorphan. Dawson, GS; Ramadan, HH; Seidman, P, 2001)	1.98
"Dextromethorphan (DXM) is a widely used probe drug for human CYP2D6 activity both in vitro and in vivo. "	( Comparative contribution to dextromethorphan metabolism by cytochrome P450 isoforms in vitro: can dextromethorphan be used as a dual probe for both CTP2D6 and CYP3A activities? Haining, RL; Yu, A, 2001)	2.05
"Dextromethorphan (DXM) is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist shown to prevent the development of tolerance to the antinociceptive effects of morphine in rodents. "	( Dextromethorphan potentiates the antinociceptive effects of morphine and the delta-opioid agonist SNC80 in squirrel monkeys. Allen, RM; Dykstra, LA; Granger, AL, 2002)	3.2
"Dextromethorphan is a probe substrate to determine CYP2D6 phenotype. "	( Development of a rapid and sensitive high-performance liquid chromatographic method to determine CYP2D6 phenotype in human liver microsomes. March, C; Rege, B; Sarkar, MA, 2002)	1.76
"Dextromethorphan (DM) is a neuroprotective agent. "	( Nasal delivery of [14C]dextromethorphan hydrochloride in rats: levels in plasma and brain. Behl, CR; Char, H; Iqbal, K; Kumar, S; Malick, AW; Patel, S; Piemontese, D; Salvador, RA, 1992)	2.04
"Dextromethorphan is a highly effective and widely used nonopioid antitussive drug. "	( Dextromethorphan. An overview of safety issues. Bem, JL; Peck, R, )	3.02
"Dextromethorphan (DM) is an antitussive with anticonvulsant activity that binds to high- and low-affinity sites in guinea pig brain homogenates. "	( Autoradiographic localization of [3H]dextromethorphan in guinea pig brain: allosteric enhancement by ropizine. Canoll, PD; Gottesman, S; Musacchio, JM; Smith, PR, 1989)	1.99

Excerpt	Reference	Relevance
"Dextromethorphan (DXM) has been re-purposed several times over the past 7 decades: first as a cough suppressant, then as a compounded formulation with quinidine for treatment of pseudobulbar affect, and most recently as a compounded formulation with bupro-pion for treatment of major depressive disorder. "	( Dextromethorphan: From Cough Suppressant to Antidepressant. Kverno, K, 2022)	3.61
"Dextromethorphan has been used as an abortive and prophylactic treatment for MTX-NT."	( Dextromethorphan Administration on Day 0 and Day 7 for Secondary Prevention of Methotrexate-induced Neurotoxicity in Childhood Acute Lymphoblastic Leukemia: A Retrospective Case Series. Fustino, NJ; Juhl, K; Leister, J, 2021)	2.79
"Dextromethorphan (DM) has been reported to possess neuroprotective effects in lipopolysaccharide- (LPS-) stimulated animals; however, it remains unclear whether epigenetic regulatory mechanisms in microglial cells are involved in such DM-mediated neuroprotective effects."	( Dextromethorphan Suppresses Lipopolysaccharide-Induced Epigenetic Histone Regulation in the Tumor Necrosis Factor- Kuo, KC; Wu, PL; Yang, CH; Yang, SN; Yang, YN; Yang, YSH, 2020)	2.72
"Dextromethorphan (DXM) has overtaken codeine as the most widely used cough suppressant due to its availability, efficacy, and safety profile at directed doses."	( Dextromethorphan in Cough Syrup: The Poor Man's Psychosis. Birur, B; Black, JR; Bolis, RA; Fargason, RE; Martinak, B, 2017)	2.62
"Dextromethorphan and memantine have been administered to animals after spinal nerve ligation (SNL) to evaluate their antinociceptive/cognitive effects and associated molecular events, including the phosphorylation of several tyrosine (pTyr(1336), pTyr(1472)) residues in the NR2B NMDAR subunit."	( Low doses of dextromethorphan have a beneficial effect in the treatment of neuropathic pain. Chalus, M; Daulhac, L; Dupuis, A; Eschalier, A; Etienne, M; Morel, V; Pickering, G; Privat, AM, 2014)	1.49
"Dextromethorphan has been reported to ameliorate opioid withdrawal symptoms in both animal and human subjects. "	( A double-blind, placebo-controlled trial of dextromethorphan combined with clonidine in the treatment of heroin withdrawal. Chen, CH; Lin, SK; Pan, CH, 2014)	2.11
"Dextromethorphan (DM) has been used for more than 50years as an over-the-counter antitussive. "	( Pharmacology of dextromethorphan: Relevance to dextromethorphan/quinidine (Nuedexta®) clinical use. Matsumoto, RR; Pope, LE; Siffert, J; Taylor, CP; Traynelis, SF, 2016)	2.22
"Dextromethorphan (DM) has been well-characterized as a neuroprotective agent in experimental models of CNS injury. "	( Neuroprotective profile of dextromethorphan in an experimental model of penetrating ballistic-like brain injury. Lu, XC; Sharrow, K; Shear, DA; Tortella, FC; Williams, AJ, 2009)	2.09
"Dextromethorphan (DXM) has unique toxicity that may be difficult to diagnose. "	( Dextromethorphan abuse masquerading as a recurrent seizure disorder. Ali, SS; Lee, DC; Majlesi, N, 2011)	3.25
"Dextromethorphan (DM) has been shown to protect against endotoxic shock in mice. "	( Attenuating heat-induced acute lung inflammation and injury by dextromethorphan in rats. Chang, CP; Hou, CC; Lin, MT; Yang, HH, 2012)	2.06
"Dextromethorphan at high doses has phencyclidine-like effects on the NMDA receptor system; recreational use of high doses has been found to cause mania and hallucinations."	( Dextromethorphan abuse leading to assault, suicide, or homicide. Frost, MP; Goldfogel, G; Logan, BK; Sandstrom, G; Wickham, DJ; Yeakel, JK, 2012)	2.54
"Dextromethorphan has been reported to decrease the self-administration of several drugs of abuse, including morphine, methamphetamine, cocaine, and nicotine. "	( Effects of dextromethorphan on dopamine release in the nucleus accumbens: Interactions with morphine. Glick, SD; Maisonneuve, IM; Steinmiller, CL, 2003)	2.15
"Dextromethorphan has moderate affinities for phencyclidine sites, while dimemorfan has very low affinities for such sites, suggesting that these sites are not essential for the anticonvulsant actions of dimemorfan."	( The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan. Cha, JY; Chen, CF; Jhoo, WK; Kim, HC; Kim, WK; Ko, KH; Lim, YK; Nah, SY; Shin, EJ, 2005)	1.61
"Dextromethorphan has been used as an antitussive for more than 40 years and is considered a drug with a good margin of safety. "	( Dextromethorphan, 3-methoxymorphinan, and dextrorphan have local anaesthetic effect on sciatic nerve blockade in rats. Chen, YW; Hou, CH; Lin, CN; Lin, MT; Tu, CH; Tzeng, JI; Wang, JJ, 2006)	3.22
"Dextromethorphan has been reported to be a weak antagonist of the ion channel associated with the NMDA receptor, and to have putative antiparkinsonian activity in man. "	( Antiparkinsonian action of dextromethorphan in the reserpine-treated mouse. Kaur, S; Starr, MS, 1995)	2.03
"Dextromethorphan has been shown to protect against ischemic tissue damage. "	( Dextromethorphan attenuates the effects of ischemia on rabbit electroretinographic oscillatory potentials. Brunette, JR; Cao, W; Drumheller, A; Jolicoeur, FB; Lafond, G; Zaharia, M, 1993)	3.17
"Dextromethorphan has analgesic efficacy in the experimental formalin test, blocks the nociceptive activation of the immediate-early gene, c-fos proto-oncogene, and prevents and reverses the development of opiate analgesic tolerance in experimental models."	( Dextromethorphan shows efficacy in experimental pain (nociception) and opioid tolerance. Brodsky, M; Elliott, KJ; Foley, KM; Hyanansky, A; Inturrisi, CE, 1995)	2.46
"Dextromethorphan (DM) has been observed to afford neuroprotection in a variety of in vitro and in vivo experimental models of CNS injury. "	( Dextromethorphan protects against cerebral injury following transient, but not permanent, focal ischemia in rats. Britton, P; Laskosky, MS; Lu, XC; Tortella, FC, 1997)	3.18
"Dextromethorphan has been on the market for many years and has never been implicated as a human teratogen."	( Dextromethorphan. Extrapolation of findings from reproductive studies in animals to humans. Einarson, A; Koren, G, 1999)	2.47
"Dextromethorphan has been proposed as a test compound to assess drug oxidation polymorphism."	( Effect of liver disease on dextromethorphan oxidation capacity and phenotype: a study in 107 patients. Amouyal, G; Babany, G; Freneaux, E; Habersetzer, F; Larrey, D; Letteron, P; Pessayre, D; Tinel, M, 1989)	1.3

Excerpt	Reference	Relevance
"Dextromethorphan produced lower ED(50) values for morphine, fentanyl and sufentanil but exerted no effect on the potency of SNC80 or U50,488H."	( Dextromethorphan and ketamine potentiate the antinociceptive effects of mu- but not delta- or kappa-opioid agonists in a mouse model of acute pain. Baker, AK; Hoffmann, VL; Meert, TF, 2002)	2.48
"Dextromethorphan produced lower ED50 values for morphine, fentanyl and sufentanil but exerted no effect on SNC80 or U50,488H."	( Interactions of NMDA antagonists and an alpha 2 agonist with mu, delta and kappa opioids in an acute nociception assay. Baker, AK; Hoffmann, VL; Meert, TF, 2002)	1.04
"Dextromethorphan can produce psychoactive effects similar to that of marijuana, and higher doses will produce dissociative effects, including sensory enhancement and hallucinations."	( Dextromethorphan in Wisconsin drivers. Cochems, A; Harding, P; Liddicoat, L, 2007)	2.5
"Dextromethorphan can produce serotonin syndrome in the absence of another serotonergic drug."	( Serotonin syndrome in dextromethorphan ingestion responsive to propofol therapy. Babu, KM; Boyer, EW; Ganetsky, M, 2007)	1.38

Excerpt	Reference	Relevance
"The dextromethorphan-treated rats were given 12, 24 and 48 mg/kg (low, medium, high) of dextromethorphan by intragastric administration each day for 3 days."	( Serum metabolic changes in rats after intragastric administration of dextromethorphan. Bao, S; Chen, L; Hong, L; Hu, L; Lin, G; Lin, Z; Mo, J; Qian, S; Su, K; Sun, F; Wang, X; Wen, C; Wu, Q; Zhang, J, 2017)	1.17
"Dextromethorphan pretreatment significantly suppressed the production of tumour necrosis factor-alpha, monocyte chemoattractant protein-1, interleukin-6, interleukin-10, and superoxide in macrophage cell culture after stimulation."	( Dextromethorphan reduces oxidative stress and inhibits atherosclerosis and neointima formation in mice. Hong, JS; Huang, CW; Jiang, SJ; Li, YH; Liu, PY; Liu, SL; Shi, GY; Tang, SH; Wu, HL, 2009)	2.52
"Dextromethorphan treatment induced a slight inhibition of peak currents in human K(v)1.2 and K(v)1.3 channels, whereas dextromethorphan profoundly inhibited the steady-state currents of human K(v)1.3 channels compared to K(v)1.2 channel currents."	( Effect of dextromethorphan on human K(v)1.3 channel activity: involvement of C-type inactivation. Choi, SH; Hwang, SH; Kim, HC; Lee, BH; Lee, JH; Nah, SY; Shin, TJ, 2011)	1.49
"Dextromethorphan treatment led to a significant but modest reduction in morphine requirements (29.3% P < 0.05) but no reduction in postoperative pain levels."	( Large-dose oral dextromethorphan as an adjunct to patient-controlled analgesia with morphine after knee surgery. Clarke, D; Goodchild, CS; Wadhwa, A; Young, D, 2001)	1.38
"Dextromethorphan-treated patients reported significantly (p < 0.05) less pain and sedation, and felt better."	( Combined pre-incisional oral dextromethorphan and epidural lidocaine for postoperative pain reduction and morphine sparing: a randomised double-blind study on day-surgery patients. Ben-Abraham, R; Flaishon, R; Lalayev, G; Niv, D; Weinbroum, AA; Yashar, T, 2001)	1.32
"Dextromethorphan-treated animals (n = 10) showed less lactate formation during ischemia than untreated animals (n = 11, p less than 0.001)."	( Effects of dextromethorphan on rat brain during ischemia and reperfusion assessed by magnetic resonance spectroscopy. Balázs, R; Lewis, P; Nasim, MM; Tulleken, CA; van Echteld, CJ; van Rijen, PC; Verheul, HB, 1991)	1.39
"Dextromethorphan-pretreated animals required a significantly larger dose of PTZ than did controls to produce the first myoclonic jerk, but a significantly smaller dose of the convulsant to produce maximal seizures."	( Effect of orally administered dextromethorphan on theophylline- and pentylenetetrazol-induced seizures in rats. Levy, G; Zhi, JG, 1990)	1.29
"The dextromethorphan-treated rabbits also demonstrated significantly smaller areas of cortical edema (10.2%) on magnetic resonance imaging than the controls (38.6%, p less than 0.01)."	( Dextromethorphan protects against cerebral injury following transient focal ischemia in rabbits. DeLaPaz, R; George, CP; Gross, T; Shibata, DK; Steinberg, GK, 1988)	2.2
"Treatment of dextromethorphan 1 with various alkylating agents followed by base treatment led to Hoffman-type elimination reactions to produce a series of tricyclic derivatives, 6. "	( Synthesis of potent sigma-1 receptor ligands via fragmentation of dextromethorphan. Arrington, MP; Brown, C; Schwartz, CE, 2004)	0.93
"Treatment of dextromethorphan (32 mg/kg) alone or in combination with CYP2D6 enzyme inhibitor Quinidine (32 mg/kg) failed to produce rapid antidepressant-like effects by increasing the latency to drink in the NIH test rather than decreasing the latency to drink."	( Assessment of the rapid and sustained antidepressant-like effects of dextromethorphan in mice. Garrett, PI; Hillhouse, TM; Honeycutt, SC; Peterson, AM; Saavedra, JS; White, JW, 2020)	1.15
"Treatment with Dextromethorphan/Quinidine (DM/Q) has demonstrated benefit on pseudobulbar affect and bulbar function in amyotrophic lateral sclerosis (ALS). "	( Effect of one-year dextromethorphan/quinidine treatment on management of respiratory impairment in amyotrophic lateral sclerosis. Burés, E; Ferrer, S; Luis Díaz, J; Sancho, J; Servera, E; Signes-Costa, J; Torrecilla, T, 2021)	1.3
"Pretreatment with dextromethorphan (20 mg/kg s.c., 20 min prior) potentiated the effects of acute morphine, while attenuating the effects of chronic morphine on nucleus accumbens DA levels."	( Effects of dextromethorphan on dopamine release in the nucleus accumbens: Interactions with morphine. Glick, SD; Maisonneuve, IM; Steinmiller, CL, 2003)	1.03
"Pretreatment with dextromethorphan at 60 mg/kg s.c., 30 min prior to formalin resulted in a suppression of c-fos induction, so that c-fos mRNA levels in the ipsilateral spinal dorsal horn of animals receiving dextromethorphan prior to formalin did not differ from controls."	( Dextromethorphan suppresses both formalin-induced nociceptive behavior and the formalin-induced increase in spinal cord c-fos mRNA. Brodsky, M; Elliott, KJ; Foley, KM; Hynansky, AD; Inturrisi, CE, 1995)	2.06
"Treatment with dextromethorphan, an NMDA receptor antagonist, was started between 48 hours and 14 days after the critical incident."	( Drug refractory epilepsy in brain damage: effect of dextromethorphan on EEG in four patients. Baumann, P; Boltshauser, E; Fanconi, S; Netzer, R; Schmitt, B, 1994)	0.88
"Treatment with dextromethorphan or levemopamil reduced the deficit in spatial learning by limiting the increase in swim distance due to ischemia."	( Global ischemic neuronal damage relates to behavioural deficits: a pharmacological approach. Block, F; Schwarz, M, 1998)	0.64
"Pretreatment with dextromethorphan was associated with a significant decrease in the concentrations of theophylline in the cerebrospinal fluid and serum at the pharmacologic endpoint."	( Effect of orally administered dextromethorphan on theophylline- and pentylenetetrazol-induced seizures in rats. Levy, G; Zhi, JG, 1990)	0.89

Excerpt	Reference	Relevance
" An anthology of adverse drug events has been analysed, drawn both from published case records and a data base recording dextromethorphan-related adverse events spontaneously reported by physicians or pharmacists."	( Dextromethorphan. An overview of safety issues. Bem, JL; Peck, R, )	1.78
" A literature review, brief review of pharmacology, and report of two cases of adverse reactions to dextromethorphan-containing preparations are presented."	( Toxicity with dextromethorphan-containing preparations: a literature review and report of two additional cases. Parks, BR; Pender, ES, 1991)	0.86
" They were given individually to guinea pigs prior to poisoning with 2 x LD50 soman to test their efficacy against organophosphorus-induced convulsions, brain damage, and lethality."	( Prevention of soman neurotoxicity by non-opioid antitussives. Braitman, DJ; Brennecke, LH; Sparenborg, S, 1990)	0.28
"The anticonvulsant and adverse effects of dextromethorphan, a non-opioid antitussive, and its metabolite dextrorphan were examined in amygdala-kindled rats."	( Differences in anticonvulsant potency and adverse effects between dextromethorphan and dextrorphan in amygdala-kindled and non-kindled rats. Hönack, D; Löscher, W, 1993)	0.79
" All symptoms were reversible and no patient suffered severe adverse reactions."	( Dose escalation safety and tolerance study of the N-methyl-D-aspartate antagonist dextromethorphan in neurosurgery patients. Bell, TE; Steinberg, GK; Yenari, MA, 1996)	0.52
"Extracellular levels of endogenous glutamate are relatively high in the developing rabbit retina but nonetheless appear to promote cell survival and developmental processes at concentrations considered toxic in the adult."	( N-methyl-D-aspartate-mediated glutamate toxicity in the developing rabbit retina. Haberecht, MF; Lo, GJ; Mitchell, CK; Redburn, DA, 1997)	0.3
" Slow DM metabolizers took significantly lower daily doses of MorphiDex than rapid metabolizers without a significant difference in the incidence of adverse events."	( Long-term safety of MorphiDex. Goldblum, R, 2000)	0.31
"In this study, we have focused our investigation of the facts whether co-administration of a NMDA antagonist dextromethorphan (DM) with morphine during pregnancy and throughout lactation could prevent the adverse effects associated with chronic morphine administration in rat offspring."	( Co-administration of dextromethorphan during pregnancy and throughout lactation significantly decreases the adverse effects associated with chronic morphine administration in rat offspring. Su, CH; Tao, PL; Wu, YH; Yeh, GC, 2001)	0.84
" Hcy is directly toxic to vascular endothelium and it and its metabolites are excitatory agonists of the N-methyl-D-aspartate (NMDA) receptor."	( Dextromethorphan is effective in the treatment of subacute methotrexate neurotoxicity. Aisner, J; Cole, PD; Drachtman, RA; Golden, CB; James, SJ; Kamen, BA; Melnyk, S, )	1.57
" Participants in the DM group reported many more adverse events than did subjects on placebo (173 vs."	( A randomized, double-blind, placebo-controlled safety study of high-dose dextromethorphan in methadone-maintained male inpatients. Bead, V; Caruso, FS; Childress, AR; Cornish, JW; Ehrman, RN; Esmonde, CA; Herman, BH; Martz, K; O'Brien, CP; Poole, S; Robbins, SJ, 2002)	0.55
" However, there have been reports of patients experiencing adverse events with related agents."	( Safety of selegiline with cold medications. Jacob, JE; Sage, JI; Wagner, ML, 2003)	0.32
" If selegiline is used with these medications, watch for adverse events or replace selegiline with another drug."	( Safety of selegiline with cold medications. Jacob, JE; Sage, JI; Wagner, ML, 2003)	0.32
"Dextromethorphan (DEM) shares part of the adverse event profile of opioids and is widely used as a probe drug for CYP2D6 phenotyping and for the assessment of CYP2D6 activity."	( Measurement of CYP2D6 and CYP3A4 activity in vivo with dextromethorphan: sources of variability and predictors of adverse effects in 419 healthy subjects. Becquemont, L; Boëlle, PY; Bornert, C; Funck-Brentano, C; Poirier, JM; Verstuyft, C, 2005)	2.02
" Logistic regression was performed to examine the factors associated with changes in metabolic ratios and with the occurrence of adverse events."	( Measurement of CYP2D6 and CYP3A4 activity in vivo with dextromethorphan: sources of variability and predictors of adverse effects in 419 healthy subjects. Becquemont, L; Boëlle, PY; Bornert, C; Funck-Brentano, C; Poirier, JM; Verstuyft, C, 2005)	0.58
" Based on multivariate analysis, the CYP2D6 metabolic ratio was a stronger independent predictor of adverse events (p<0."	( Measurement of CYP2D6 and CYP3A4 activity in vivo with dextromethorphan: sources of variability and predictors of adverse effects in 419 healthy subjects. Becquemont, L; Boëlle, PY; Bornert, C; Funck-Brentano, C; Poirier, JM; Verstuyft, C, 2005)	0.58
" The CYP2D6 metabolic ratio predicts adverse events to DEM as does CYP2D6 phenotype, and extensive metabolizer subjects are not protected against adverse events."	( Measurement of CYP2D6 and CYP3A4 activity in vivo with dextromethorphan: sources of variability and predictors of adverse effects in 419 healthy subjects. Becquemont, L; Boëlle, PY; Bornert, C; Funck-Brentano, C; Poirier, JM; Verstuyft, C, 2005)	0.58
" Adverse effects of these medications and the lack of evidence of their efficacy in children make their use a serious matter."	( Toxicity and use of over-the-counter cough and cold medication in the pediatric population. Montgomery, EJ; Wasserman, GS, )	0.13
"3,4-Methylenedioxymethamphetamine (MDMA)'s O-demethylenated metabolite, 3,4-dihydroxymethamphetamine (HHMA), has been hypothesized to serve as a precursor for the formation of toxic catechol-thioether metabolites (e."	( Inhibition of 3,4-methylenedioxymethamphetamine metabolism leads to marked decrease in 3,4-dihydroxymethamphetamine formation but no change in serotonin neurotoxicity: implications for mechanisms of neurotoxicity. Maldonado Adrian, C; McCann, UD; Mueller, M; Ricaurte, GA; Yuan, J, 2011)	0.37
" Adverse events were mostly mild or moderate and of expected types."	( Efficacy and safety of dextromethorphan/quinidine at two dosage levels for diabetic neuropathic pain: a double-blind, placebo-controlled, multicenter study. Hepner, A; Pope, LE; Shaibani, AI; Thisted, R, 2012)	0.69
" Safety measures included adverse events (AEs), laboratory tests, electrocardiograms (ECGs), vital signs, and physical examinations."	( An open-label multicenter study to assess the safety of dextromethorphan/quinidine in patients with pseudobulbar affect associated with a range of underlying neurological conditions. Appel, SH; Formella, AE; Lomen-Hoerth, C; Pattee, GL; Pope, LE; Wymer, JP, 2014)	0.65
" Adverse events included headache (7."	( An open-label study to assess safety, tolerability, and effectiveness of dextromethorphan/quinidine for pseudobulbar affect in dementia: PRISM II results. Cutler, AJ; D'Amico, S; Davis, CS; Doody, RS; Ledon, F; Shin, P; Siffert, J; Yonan, C, 2016)	0.67
"DM/Q significantly reduced PBA symptoms in patients with dementia; reported adverse events were consistent with the known safety profile of DM/Q."	( An open-label study to assess safety, tolerability, and effectiveness of dextromethorphan/quinidine for pseudobulbar affect in dementia: PRISM II results. Cutler, AJ; D'Amico, S; Davis, CS; Doody, RS; Ledon, F; Shin, P; Siffert, J; Yonan, C, 2016)	0.67
" We sought to characterize adverse events associated with dextromethorphan in children <12 years old from a surveillance program of OTC cough/cold medication exposures."	( Adverse events associated with pediatric exposures to dextromethorphan. Banner, W; Bond, GR; Burnham, RI; Green, JL; Kauffman, RE; Palmer, RB; Paul, IM; Reynolds, KM, 2017)	0.95
"1716 cases contained ≥1 adverse event deemed at least potentially related to dextromethorphan; 1417 were single product exposures."	( Adverse events associated with pediatric exposures to dextromethorphan. Banner, W; Bond, GR; Burnham, RI; Green, JL; Kauffman, RE; Palmer, RB; Paul, IM; Reynolds, KM, 2017)	0.93
" Adverse events were predominantly associated with overdose, most commonly affecting the central nervous and autonomic systems."	( Adverse events associated with pediatric exposures to dextromethorphan. Banner, W; Bond, GR; Burnham, RI; Green, JL; Kauffman, RE; Palmer, RB; Paul, IM; Reynolds, KM, 2017)	0.7
" Adverse events (AEs) were consistent with the known DM/Q safety profile; the most common AE was diarrhea (8."	( Safety, Tolerability, and Effectiveness of Dextromethorphan/Quinidine for Pseudobulbar Affect Among Study Participants With Traumatic Brain Injury: Results From the PRISM-II Open Label Study. Davis, C; Formella, AE; Hammond, FM; Ledon, F; Sauve, W, 2018)	0.74
"Initial research following regulatory changes addressing the pediatric safety of cough and cold medications (CCMs) demonstrated decreases in adverse events (AEs)."	( Trends in adverse events and related health-care facility utilization from cough and cold medication exposures in children. Banner, W; Bond, GR; Dart, RC; Green, JL; Kauffman, RE; Palmer, RB; Paul, IM; Rapp-Olsson, M; Reynolds, KM; Wang, GS, 2021)	0.62
" No serious adverse events/deaths were reported."	( Napabucasin Drug-Drug Interaction Potential, Safety, Tolerability, and Pharmacokinetics Following Oral Dosing in Healthy Adult Volunteers. Brantley, SJ; Dai, X; Goulet, MT; Hard, ML; Hitron, M; Karol, MD; McLaughlin, CF, 2021)	0.62
" The treatment was well-tolerated, with some transient adverse events reported."	( Dextromethorphan-Bupropion for the Treatment of Depression: A Systematic Review of Efficacy and Safety in Clinical Trials. Akbar, D; Cao, B; Ceban, F; Ho, R; Kwan, ATH; McIntyre, RS; Rhee, TG; Rosenblat, JD; Subramaniapillai, M; Teopiz, KM, 2023)	2.35

Excerpt	Reference	Relevance
" To examine whether this effect is related to the chemical structure or pharmacokinetic characteristics of the inhibiting agent, we determined the effect of dextromethorphan (a compound which exhibits pharmacokinetic similarities to, but is chemically dissimilar from, previously studied agents) on the disposition of antipyrine."	( Dextromethorphan pretreatment induces antipyrine clearance in the rat. Svensson, CK; Ware, JA, 1988)	1.91
" No therapeutically significant differences were detected between the three preparations tested, and there were no great differences between the pharmacokinetic profiles of dextromethorphan and dextrorphan."	( Pharmacokinetics of dextromethorphan and dextrorphan: a single dose comparison of three preparations in human volunteers. Hänninen, U; Karttunen, P; Kokkonen, P; Nykänen, S; Silvasti, M; Tukiainen, H, 1987)	0.79
" Detailed pharmacokinetic and neuropsychology studies were performed."	( High-dose dextromethorphan in amyotrophic lateral sclerosis: phase I safety and pharmacokinetic studies. Evans, WE; Hollander, D; Kaplan, R; McLeod, HL; Munsat, TL; Pradas, J, 1994)	0.69
"The pharmacokinetic interactions of sertraline and fluoxetine with the tricyclic antidepressant desipramine were studied in 18 healthy male volunteers phenotyped as extensive metabolizers of dextromethorphan."	( Pharmacokinetics of desipramine coadministered with sertraline or fluoxetine. Alderman, J; Chung, M; Harris, S; Harrison, W; Messig, M; Preskorn, SH, 1994)	0.48
"The present report describes the pharmacokinetic characteristics of dextromethorphan (DM) and its main active metabolite dextrorphan (DX) in a group of epileptic patients receiving comedication."	( Pharmacokinetics of dextromethorphan and dextrorphan in epileptic patients. Kazis, A; Kimiskidis, V; Niopas, I, )	0.69
" No evidence was seen of a pharmacokinetic interaction between CIT and Li, and this combination was well tolerated."	( A double-blind, placebo-controlled study of citalopram with and without lithium in the treatment of therapy-resistant depressive patients: a clinical, pharmacokinetic, and pharmacogenetic investigation. Amey, M; Baettig, D; Baumann, P; Jonzier-Perey, M; Kasas, A; Lambert, S; Montaldi, S; Nil, R; Souche, A; Uehlinger, C, 1996)	0.29
" For the 200 mg dose group, the single dose plasma results showed no significant differences in pharmacokinetic parameters for NEF and HO-NEF in EM compared with PM subjects."	( Single and multiple dose pharmacokinetics of nefazodone in subjects classified as extensive and poor metabolizers of dextromethorphan. Barbhaiya, RH; Buch, AB; Greene, DS, 1996)	0.5
"5 mg/kg in a crossover fashion in a two-sequence pharmacokinetic study with a wash-out period of at least 7 days."	( A urine metabolic ratio of dextromethorphan and 3-methoxymorphinan as a probe for CYP3A activity and prediction of cyclosporine clearance in healthy volunteers. Fleckenstein, LL; Ku, YM; Min, DI; Vichiendilokkul, A, 1999)	0.6
" The enhancement of MS analgesia by DM is due to a pharmacodynamic interaction, not an effect on MS blood levels or a pharmacokinetic interaction between MS and DM, or their metabolites."	( MorphiDex pharmacokinetic studies and single-dose analgesic efficacy studies in patients with postoperative pain. Caruso, FS, 2000)	0.31
"The terminal half-life of sabeluzole was significantly prolonged in subjects with severe hepatic dysfunction vs healthy subjects (respectively 39."	( Pharmacokinetics of sabeluzole and dextromethorphan oxidation capacity in patients with severe hepatic dysfunction and healthy volunteers. Blin, O; Bouhours, P; Lacarelle, B; Le Moing, JP; Levron, JC; Micallef, J; Nataf, MB; Pageaux, GP, 2001)	0.59
" The authors present data evaluating the pharmacokinetic and pharmacodynamic responses to coadministration of oral linezolid with sympathomimetics (pseudoephedrine and phenylpropanolamine) and a serotonin reuptake inhibitor (dextromethorphan)."	( Linezolid: pharmacokinetic and pharmacodynamic evaluation of coadministration with pseudoephedrine HCl, phenylpropanolamine HCl, and dextromethorpan HBr. Antal, EJ; Batts, DH; Hendershot, PE; Hopkins, NK; Welshman, IR, 2001)	0.5
" An analysis of pharmacokinetic parameters for determining the DM metabolic phenotype was conducted."	( Analysis of pharmacokinetic parameters for assessment of dextromethorphan metabolic phenotypes. Chen, JY; Ho, HO; Lee, YJ; Sheu, MT; Tao, PL; Yeh, GC, )	0.38
" A multiple-dose study in healthy subjects with an extensive or a poor enzyme metabolizer phenotype evaluated the safety and pharmacokinetic profile of a selected fixed-dose combination (AVP-923)."	( Pharmacokinetics of dextromethorphan after single or multiple dosing in combination with quinidine in extensive and poor metabolizers. Berg, JE; Khalil, MH; Pope, LE; Sellers, EM; Stiles, M; Yakatan, GJ, 2004)	0.65
" The pharmacokinetic parameters of dextrorphan were calculated by non-compartment model statistics."	( [Determination of dextrorphan in human plasma and pharmacokinetic study]. Chen, XY; Gu, Q; Liu, D; Zhang, Y; Zhang, YF; Zhong, DF, 2004)	0.32
" Pharmacokinetic parameters of dextrorphan was obtained as follows: Tmax was (2."	( [Determination of dextrorphan in human plasma and pharmacokinetic study]. Chen, XY; Gu, Q; Liu, D; Zhang, Y; Zhang, YF; Zhong, DF, 2004)	0.32
") on hyperalgesia and pain after a tissue injury in human volunteers, and to describe the relationship between pharmacokinetic and pharmacodynamic data."	( Intravenous dextromethorphan to human volunteers: relationship between pharmacokinetics and anti-hyperalgesic effect. Dahl, JB; Dirks, J; Duedahl, TH; Larsen, NE; Petersen, KB; Romsing, J, 2005)	0.71
" Whereas 6 subjects of each phenotype were adequate to achieve 80% power in showing pharmacokinetic differences, the power required to detect a difference in antitussive response was less than 80% with 500 subjects in each study arm."	( Incorporating in vitro information on drug metabolism into clinical trial simulations to assess the effect of CYP2D6 polymorphism on pharmacokinetics and pharmacodynamics: dextromethorphan as a model application. Dickinson, GL; Lennard, MS; Proctor, NJ; Rezaee, S; Rostami-Hodjegan, A; Tucker, GT, 2007)	0.53
" The enzymatic activity is reflected by various pharmacokinetic metrics such as the partial clearance of a parent compound to the respective CYP2D6-mediated metabolite or metabolic ratios."	( Evaluation of probe drugs and pharmacokinetic metrics for CYP2D6 phenotyping. Frank, D; Fuhr, U; Jaehde, U, 2007)	0.34
" Pharmacokinetic parameters of midazolam and dextromethorphan were assessed alone and in the presence of AMD070."	( Pharmacokinetic effect of AMD070, an Oral CXCR4 antagonist, on CYP3A4 and CYP2D6 substrates midazolam and dextromethorphan in healthy volunteers. Becker, S; Calandra, GB; Chee, P; Everts, S; Hendrix, CW; MacFarland, RT; Nyunt, MM; Scarborough, R, 2008)	0.82
" Blood samples were collected periodically in both phases and analyzed for parent drugs and metabolites (dextrorphan, 4'-hydroxy-flurbiprofen and 1'-hydroxy-midazolam) to calculate pharmacokinetic parameters."	( Drug metabolism in hemorrhagic shock: pharmacokinetics of selective markers of cytochrome-P450 2C9, 2D6, and 3A4 enzyme activities in a porcine model. Beilman, GJ; Kumar, A; Mann, HJ; Remmel, RP, 2011)	0.37
" The aim of this study was to quantify the effects of the CYP2D61, 2, and *41 variants on DM metabolism in vivo and to identify other sources of pharmacokinetic variability."	( Assessment of activity levels for CYP2D61, CYP2D62, and CYP2D6*41 genes by population pharmacokinetics of dextromethorphan. Abduljalil, K; Frank, D; Fuhr, U; Gaedigk, A; Jaehde, U; Jetter, A; Kirchheiner, J; Klaassen, T; Tomalik-Scharte, D, 2010)	0.57
"The pharmacokinetic parameters and the relative bioavailability of dextromethorphan chewing gum preparation in rabbits were compared with those of the commercially available chewing dextromethorphan tablets using 3P97 software."	( [Pharmacokinetic study of a new chewing gum dextromethorphan delivery system]. Liu, BL; Liu, J; Tan, QY; Xu, ML; Zhang, JQ; Zhao, CJ, 2011)	0.87
" Pharmacokinetic analyses were performed on day 1 without sorafenib and day 28 after steady-state sorafenib exposure; sorafenib pharmacokinetics were evaluated on day 28."	( Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Flaherty, KT; Frye, RF; Lathia, C; O'Dwyer, PJ; Redlinger, M; Rosen, M; Schuchter, L, 2011)	0.37
"In the first DDI study, coadministration of ketoconazole (a CYP3A4 inhibitor) and clobazam increased clobazam's area under the concentration time curve from time zero extrapolated to infinity (AUC(0-∞) ) 54% and decreased clobazam's maximum plasma concentration (C(max) ) by 15% versus administration of clobazam alone, but the combination affected these pharmacokinetic parameters for N-CLB to a lesser degree."	( Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Bekersky, I; Blum, RA; Tolbert, D; Walzer, M, 2012)	0.38
" The method has high sensitivity, specificity and allows high throughput analysis required for a pharmacokinetic study."	( Simultaneous determination of dextromethorphan, dextrorphan and doxylamine in human plasma by HPLC coupled to electrospray ionization tandem mass spectrometry: application to a pharmacokinetic study. De Nucci, G; Donato, JL; Koizumi, F; Mendes, GD; Pereira, AS, 2012)	0.67
" Pharmacokinetic blood sampling was performed to assess the primary endpoints of the 90% confidence intervals (CIs) for the geometric mean ratios of the areas under the plasma concentration-time curves (AUCs) for memantine, dextromethorphan, dextrorphan - the dextromethorphan metabolite - and quinidine during concomitant therapy versus monotherapy."	( A study of potential pharmacokinetic and pharmacodynamic interactions between dextromethorphan/quinidine and memantine in healthy volunteers. Bartlett, C; Pope, LE; Schoedel, KA; Sellers, EM, 2012)	0.79
"25) for memantine, dextromethorphan and dextrorphan, indicating no pharmacokinetic DDI."	( A study of potential pharmacokinetic and pharmacodynamic interactions between dextromethorphan/quinidine and memantine in healthy volunteers. Bartlett, C; Pope, LE; Schoedel, KA; Sellers, EM, 2012)	0.94
"Minimal pharmacokinetic and pharmacodynamic interactions were observed between memantine and DMQ, suggesting they can be coadministered without dose adjustment."	( A study of potential pharmacokinetic and pharmacodynamic interactions between dextromethorphan/quinidine and memantine in healthy volunteers. Bartlett, C; Pope, LE; Schoedel, KA; Sellers, EM, 2012)	0.61
" The developed method was successfully applied to analyze the drug in samples of rat plasma for pharmacokinetic study."	( Simultaneous determination of dextromethorphan and dextrophan in rat plasma by LC-MS/MS and its application to a pharmacokinetic study. Chen, X; Hu, L; Wang, X; Wang, Z; Xu, R; Xu, T; Zhan, H; Zhang, X, 2012)	0.67
" In contrast, there were no significant differences in any of the pharmacokinetic parameters for warfarin between the two genotypes."	( Pharmacogenomic/pharmacokinetic assessment of a four-probe cocktail for CYPs and OATPs following oral microdosing. Ando, Y; Deguchi, M; Fukae, M; Hirota, T; Ieiri, I; Irie, S; Iwasaki, K; Kanda, E; Kimura, M; Maeda, K; Matsuguma, K; Matsuki, S; Nakamura, T; Sugiyama, Y, 2012)	0.38
"The present study suggests that 1) the sampling strategy should be optimized according to pharmacokinetic profiles of the test drugs following oral microdosing, and 2) microdosing can be applied to the pharmacogenomic study of CYP-specific drugs."	( Pharmacogenomic/pharmacokinetic assessment of a four-probe cocktail for CYPs and OATPs following oral microdosing. Ando, Y; Deguchi, M; Fukae, M; Hirota, T; Ieiri, I; Irie, S; Iwasaki, K; Kanda, E; Kimura, M; Maeda, K; Matsuguma, K; Matsuki, S; Nakamura, T; Sugiyama, Y, 2012)	0.38
"We conducted a pharmacokinetic (PK) study and a pharmacodynamic (PD) study to assess whether Roux-en-Y gastric bypass (RYGB) surgery is associated with significant changes to PK and PD of oral medications."	( Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients. Chalasani, N; Hall, SD; Jones, DR; Mattar, S; Tandra, S; Vuppalanchi, R, 2013)	0.39
" Compared with controls, the RYGB group had brisk natriuresis, with significantly lower tmax for urine sodium (1."	( Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients. Chalasani, N; Hall, SD; Jones, DR; Mattar, S; Tandra, S; Vuppalanchi, R, 2013)	0.39
"RYGB recipients have significantly shorter tmax for the studied orally administered medications, but otherwise no other significant changes in PK were reported."	( Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients. Chalasani, N; Hall, SD; Jones, DR; Mattar, S; Tandra, S; Vuppalanchi, R, 2013)	0.39
"Conducting pharmacokinetic (PK) studies in pregnant women is challenging."	( A physiologically based pharmacokinetic model to predict disposition of CYP2D6 and CYP1A2 metabolized drugs in pregnant women. Isoherranen, N; Ke, AB; Nallani, SC; Rostami-Hodjegan, A; Unadkat, JD; Zhao, P, 2013)	0.39
" To determine the clinical effect of GSE on CYP2D6, the pharmacokinetic interaction between GSE and the sensitive CYP2D6 probe dextromethorphan in healthy adult volunteers was examined."	( The effect of grape seed extract on the pharmacokinetics of dextromethorphan in healthy volunteers. Beijnen, JH; Goey, AK; Meijerman, I; Schellens, JH, 2013)	0.84
"Population pharmacokinetic models were developed for dextromethorphan, tamoxifen and their metabolites."	( Population pharmacokinetic modelling to assess the impact of CYP2D6 and CYP3A metabolic phenotypes on the pharmacokinetics of tamoxifen and endoxifen. Beijnen, JH; Binkhorst, L; de Bruijn, P; de Graan, AJ; Huitema, AD; Mathijssen, RH; ter Heine, R, 2014)	0.65
" This study determined, for the first time, the basic pharmacokinetic profile of DM and its active metabolite, dextrorphan (DP) in children and adolescents."	( Pharmacokinetic profile of dextromethorphan hydrobromide in a syrup formulation in children and adolescents. Armogida, M; Guenin, E; Riff, D, 2014)	0.7
" The terminal half-life (t ½) values were longer in the adolescent group due in part to the single PM subject."	( Pharmacokinetic profile of dextromethorphan hydrobromide in a syrup formulation in children and adolescents. Armogida, M; Guenin, E; Riff, D, 2014)	0.7
"This is the first evaluation of the pharmacokinetic characteristics of DM in children and adolescents."	( Pharmacokinetic profile of dextromethorphan hydrobromide in a syrup formulation in children and adolescents. Armogida, M; Guenin, E; Riff, D, 2014)	0.7
"To evaluate felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions (PK-DDIs) involving cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp)."	( Evaluation of felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions. Doogue, MP; Miners, JO; Polasek, TM; Rowland, A; Snyder, BD, 2014)	0.4
" Blood samples for pharmacokinetic analysis were collected pre-dose and serially for 72 h post-dose."	( Lisdexamfetamine Dimesylate Effects on the Pharmacokinetics of Cytochrome P450 Substrates in Healthy Adults in an Open-Label, Randomized, Crossover Study. Corcoran, M; Ermer, J; Martin, P, 2015)	0.42
" Plasma concentrations of slowly eliminated caffeine and R-/S-warfarin and rapidly eliminated omeprazole and midazolam previously observed in cynomolgus monkeys were scaled to human oral biomonitoring equivalents using known species allometric scaling factors and in vitro metabolic clearance data with a simple physiologically based pharmacokinetic (PBPK) model."	( Human plasma concentrations of cytochrome P450 probes extrapolated from pharmacokinetics in cynomolgus monkeys using physiologically based pharmacokinetic modeling. Murayama, N; Shida, S; Shimizu, M; Uno, Y; Utoh, M; Yamazaki, H, 2015)	0.42
" In this study, we investigated the pharmacokinetic interaction between Zuojin Pill and the sensitive CYP2D6 probe dextromethorphan in healthy Chinese volunteers with CYP2D6*10 genotype."	( Effects of the Chinese herbal formula "Zuojin Pill" on the pharmacokinetics of dextromethorphan in healthy Chinese volunteers with CYP2D6*10 genotype. Jiang, J; Liu, S; Miao, P; Qiu, F; Ye, Y; Zeng, J; Zhao, T; Zhu, L, 2016)	0.87
" In contrast, no significant change was observed in these pharmacokinetic parameters of the participants with CYP2D610/10 genotype."	( Effects of the Chinese herbal formula "Zuojin Pill" on the pharmacokinetics of dextromethorphan in healthy Chinese volunteers with CYP2D6*10 genotype. Jiang, J; Liu, S; Miao, P; Qiu, F; Ye, Y; Zeng, J; Zhao, T; Zhu, L, 2016)	0.66
" A physiologically based pharmacokinetic (PBPK) model can be developed to do simulations based on the large virtual Chinese population and evaluate single-point plasma phenotyping method of CYP2D6."	( Application of a physiologically based pharmacokinetic model for the evaluation of single-point plasma phenotyping method of CYP2D6. Berk, D; Chen, R; Hu, P; Rostami-Hodjegan, A; Shi, J; Wang, H, 2016)	0.43
"A physiologically based pharmacokinetic (PBPK) model was used to simulate the impact of elevated levels of interleukin (IL)-6 on the exposure of several orally administered cytochrome P450 (CYP) probe substrates (caffeine, S-warfarin, omeprazole, dextromethorphan, midazolam, and simvastatin)."	( Simulating the Impact of Elevated Levels of Interleukin-6 on the Pharmacokinetics of Various CYP450 Substrates in Patients with Neuromyelitis Optica or Neuromyelitis Optica Spectrum Disorders in Different Ethnic Populations. Ducray, PS; Endo-Tsukude, C; Gardner, I; Gill, KL; Hatley, OJ; Machavaram, KK; Parrott, N; Terao, K, 2019)	0.7
"The aim of this work was to predict the extent of Cytochrome P450 2D6 (CYP2D6)-mediated drug-drug interactions (DDIs) in different CYP2D6 genotypes using physiologically-based pharmacokinetic (PBPK) modeling."	( Physiologically-Based Pharmacokinetic Modeling for the Prediction of CYP2D6-Mediated Gene-Drug-Drug Interactions. Daali, Y; Desmeules, J; Storelli, F, 2019)	0.51
"This study provides a whole-body physiologically-based pharmacokinetic (PBPK) model of dextromethorphan and its metabolites dextrorphan and dextrorphan O-glucuronide for predicting the effects of cytochrome P450 2D6 (CYP2D6) drug-gene interactions (DGIs) on dextromethorphan pharmacokinetics (PK)."	( Physiologically-based pharmacokinetic modeling of dextromethorphan to investigate interindividual variability within CYP2D6 activity score groups. Fuhr, U; Lehr, T; Rüdesheim, S; Schwab, M; Selzer, D, 2022)	1.2
" This study aimed to build a physiologically based pharmacokinetic (PBPK) model reflecting observed changes in physiological and molecular parameters relevant to drug disposition that are associated with MAFLD."	( A Physiologically Based Pharmacokinetic Model to Predict the Impact of Metabolic Changes Associated with Metabolic Associated Fatty Liver Disease on Drug Exposure. Newman, EM; Rowland, A, 2022)	0.72
" The application of the method was demonstrated through the estimation of pharmacokinetic parameters that showed good congruence with earlier studies."	( Low-volume plasma sampling for determination of dextromethorphan and dextrorphan in rat plasma: LC-MS/MS method and its application in pharmacokinetic study. Ghosh, G; Kamte, S; Majhi, PK; Mishra, P; Sahu, R; Sayyad, S; Subudhi, BB, 2023)	1.17

Excerpt	Reference	Relevance
" In vivo, inhibitory potency is affected by the plasma concentration of the free (unbound) drug, a potentially important consideration since many CYP2D6-metabolised drugs exhibit nonlinear (saturable) kinetics, and by the presence of metabolites, which might accumulate and interact with the CYP system."	( Antidepressant drug interactions and the cytochrome P450 system. The role of cytochrome P450 2D6. Ereshefsky, L; Lam, YW; Riesenman, C, 1995)	0.29
"No analgesic effects of oral dextromethorphan 120 mg on pain after surgical termination of labour, and no additive analgesic effects when combined with ibuprofen 400 mg, were observed."	( The effect of dextromethorphan, alone or in combination with ibuprofen, on postoperative pain after minor gynaecological surgery. Bach, LF; Dahl, JB; Ilkjaer, S; Nielsen, PA; Wernberg, M, 2000)	0.96
" To find out whether quinidine (Q), a CYP2D6 inhibitor, could elevate and prolong DM plasma profiles, 2 multiple-dose studies identified the lowest oral dose of Q that could be used in a fixed combination with 3 doses of DM."	( Pharmacokinetics of dextromethorphan after single or multiple dosing in combination with quinidine in extensive and poor metabolizers. Berg, JE; Khalil, MH; Pope, LE; Sellers, EM; Stiles, M; Yakatan, GJ, 2004)	0.65
" The goal of this study was to investigate the effect of preincisional IM DM combined with intraoperative TEA and postoperative patient-controlled epidural analgesia (PCEA) on pain and bowel function after colonic surgery."	( Preincisional dextromethorphan combined with thoracic epidural anesthesia and analgesia improves postoperative pain and bowel function in patients undergoing colonic surgery. Huh, BK; Jao, SW; White, WD; Wong, CS; Wu, CT; Yang, CP; Yeh, CC, 2005)	0.69
"Inhibition of cytochrome P450 (CYP) is a principal mechanism for metabolism-based drug-drug interactions (DDIs)."	( Development of an in vitro drug-drug interaction assay to simultaneously monitor five cytochrome P450 isoforms and performance assessment using drug library compounds. Burdette, D; Dunklee, MB; Fahmi, O; Heinle, L; Hyland, R; Lee, C; Miller, H; Smith, D; Thurston, A; Zientek, M, )	0.13
" The method is simple, rapid and rugged, and has been applied successfully to sample analysis in support of a drug-drug interaction study."	( Simultaneous determination of tolbutamide, omeprazole, midazolam and dextromethorphan in human plasma by LC-MS/MS--a high throughput approach to evaluate drug-drug interactions. Bertelsen, K; Guo, P; Han, F; Huang, MQ; Lin, ZJ; Weng, N; Zhang, W; Zhao, H, 2010)	0.6
"25] for all analytes, indicating a drug-drug interaction."	( Randomized open-label drug-drug interaction trial of dextromethorphan/quinidine and paroxetine in healthy volunteers. Pope, LE; Schoedel, KA; Sellers, EM, 2012)	0.63
"In summary, results from this study suggest that maintenance on dextromethorphan in combination with quinidine has a limited role in the treatment of opioid dependence."	( Evaluation of the reinforcing and subjective effects of heroin in combination with dextromethorphan and quinidine. Comer, SD; Sullivan, MA; Vosburg, SK, )	0.6
"To investigate potential drug-drug interactions between clobazam and cytochrome P450 (CYP) isoenzyme substrates, inhibitors, and inducers."	( Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Bekersky, I; Blum, RA; Tolbert, D; Walzer, M, 2012)	0.38
"Two, prospective, open-label, single-center, drug-drug interaction (DDI) studies and a population pharmacokinetics analysis of seven multicenter phase II-III trials."	( Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Bekersky, I; Blum, RA; Tolbert, D; Walzer, M, 2012)	0.38
"Fifty-four healthy adult volunteers were enrolled in the two drug-drug interaction studies; 53 completed the studies."	( Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Bekersky, I; Blum, RA; Tolbert, D; Walzer, M, 2012)	0.38
"In the first drug-drug interaction study, 36 participants received a single oral dose of clobazam 10 mg on day 1, followed by either ketoconazole 400 mg once/day or omeprazole 40 mg once/day on days 17-22, with a single dose of clobazam 10 mg coadministered on day 22, to study the effects of CYP3A4 or CYP2C19 inhibition, respectively, on clobazam and its active metabolite N-desmethylclobazam (N-CLB)."	( Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Bekersky, I; Blum, RA; Tolbert, D; Walzer, M, 2012)	0.38
" In the second DDI study, no clinically significant drug-drug interactions were observed between clobazam 40 mg and the CYP probe substrates caffeine or tolbutamide."	( Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Bekersky, I; Blum, RA; Tolbert, D; Walzer, M, 2012)	0.38
"These findings suggest no clinically meaningful drug-drug interactions between clobazam and drugs metabolized by CYP3A4, CYP2C19, CYP1A2, or CYP2C9."	( Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Bekersky, I; Blum, RA; Tolbert, D; Walzer, M, 2012)	0.38
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."	( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012)	0.38
" Because of instability in plasma, further characterization of the DM1 and DM4 intramolecular and intermolecular disulfide conjugates observed in vivo is required before an accurate drug-drug interaction (DDI) prediction can be made."	( In vitro characterization of the drug-drug interaction potential of catabolites of antibody-maytansinoid conjugates. Davis, JA; Pearson, JT; Rock, DA; Wienkers, LC, 2012)	0.38
" This observed discrepancy between in vitro risk assessment and in vivo drug-drug interaction (DDI) profile was rationalized by time-varying dynamic pharmacokinetic models that incorporated circulating concentrations of fluoxetine and norfluoxetine enantiomers, mutual inhibitor-inhibitor interactions, and CYP3A4 induction."	( Fluoxetine- and norfluoxetine-mediated complex drug-drug interactions: in vitro to in vivo correlation of effects on CYP2D6, CYP2C19, and CYP3A4. Davis, C; Foti, RS; Isoherranen, N; Kunze, KL; Lutz, JD; Sager, JE, 2014)	0.4
"The objective is to explore the clinical curative effects of methylprednisolone combined with MTX and DXM intrathecal injection in treating neuropsychiatric systemic lupus erythematosus (NPSLE) and its effects on autoantibody level and anti-N-methyl-D-aspartate receptor subtype NR2a/2b antibody (anti-NR2 antibody) level."	( Impact analysis of autoantibody level and NR2 antibody level in neuropsychiatric SLE treated by methylprednisolone combined with MTX and DXM intrathecal injection. Fu, B; Lei, H; Wang, J; Zhang, J; Zhao, Y; Zhu, G, 2014)	0.4
"To evaluate felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions (PK-DDIs) involving cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp)."	( Evaluation of felodipine as a potential perpetrator of pharmacokinetic drug-drug interactions. Doogue, MP; Miners, JO; Polasek, TM; Rowland, A; Snyder, BD, 2014)	0.4
" To further validate this cocktail, in this study, we have verified whether probe drugs contained in the latter cause mutual drug-drug interactions."	( Evaluation of Mutual Drug-Drug Interaction within Geneva Cocktail for Cytochrome P450 Phenotyping using Innovative Dried Blood Sampling Method. Bosilkovska, M; Daali, Y; Déglon, J; Desmeules, J; Samer, C; Thomas, A; Walder, B, 2016)	0.43
" The study aimed to evaluate the feasibility of different doses of DXM combined with standard AM treatment in clinical hypertension."	( Combination With Low-dose Dextromethorphan Improves the Effect of Amlodipine Monotherapy in Clinical Hypertension: A First-in-human, Concept-proven, Prospective, Dose-escalation, Multicenter Study. Chen, JW; Chen, P; Cheng, SM; Hung, YJ; Tseng, WK; Wang, KY; Wen, MS; Wu, CC; Wu, TC; Yeh, HI; Yin, WH, 2016)	0.73
" In a clinical trial, a strong drug-drug interaction (DDI) was observed between dextromethorphan (DM, the object or victim drug) and GSK1034702 (the precipitant or perpetrator drug), following single and repeat doses."	( Retrospective use of PBPK modelling to understand a clinical drug-drug interaction between dextromethorphan and GSK1034702. Bloomer, J; Dear, G; Hobbs, MJ, 2017)	0.9
" The magnitude of drug-drug interaction between dextromethorphan and paroxetine was higher in homozygous than in heterozygous subjects (14."	( Impact of CYP2D6 Functional Allelic Variations on Phenoconversion and Drug-Drug Interactions. Daali, Y; Desmeules, J; Lenglet, S; Matthey, A; Storelli, F; Thomas, A, 2018)	0.74
"To evaluate the capacity for modafinil to be a perpetrator of metabolic drug-drug interactions by altering cytochrome P450 activity following a single dose and dosing to steady state."	( Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol. Mangoni, AA; Rowland, A; Sorich, MJ; van Dyk, M; Warncken, D, 2018)	0.48
"These data support consideration of the risk of clinically relevant metabolic drug-drug interactions perpetrated by modafinil when this drug is co-administered with drugs that are primarily cleared by CYP2C19 (single modafinil dose or steady state modafinil dosing) or CYP3A4 (steady state modafinil dosing only) catalysed metabolic pathways."	( Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol. Mangoni, AA; Rowland, A; Sorich, MJ; van Dyk, M; Warncken, D, 2018)	0.48
" Patients were enrolled into an inpatient study unit, and orally administered a 2 mg microdose of dextromethorphan (DM) to probe enzyme activity with and without CYP2D6-dependent drug-drug interactions."	( CYP2D6 Genotype Phenotype Discordance Due to Drug-Drug Interaction. Abbott, D; Abdelmawla, F; Anderson, PL; Bushman, LR; Flaten, HK; McDaniel, KT; Monte, AA; Saben, J; Shelton, S; West, K; Williamson, K, 2018)	0.7
" The aim of this study was to determine whether all active retinoids downregulate CYP2D6 and whether in vitro downregulation translates to in vivo drug-drug interactions (DDIs)."	( Does In Vitro Cytochrome P450 Downregulation Translate to In Vivo Drug-Drug Interactions? Preclinical and Clinical Studies With 13-cis-Retinoic Acid. Amory, JK; Hogarth, C; Isoherranen, N; Kenny, JR; Kosaka, M; Stevison, F; Wong, S, 2019)	0.51
" This study confirmed that the Inje cocktail approach was able to detect relevant drug-drug interactions impacting further development of ASP8477 and future therapeutic use."	( A Cocktail Interaction Study Evaluating the Drug-Drug Interaction Potential of the Perpetrator Drug ASP8477 at Multiple Ascending Dose Levels. Collins, C; Ernault, E; Fuhr, R; Gangaram-Panday, S; Passier, P; Treijtel, N; van Bruijnsvoort, M, 2019)	0.51
"The aim of this work was to predict the extent of Cytochrome P450 2D6 (CYP2D6)-mediated drug-drug interactions (DDIs) in different CYP2D6 genotypes using physiologically-based pharmacokinetic (PBPK) modeling."	( Physiologically-Based Pharmacokinetic Modeling for the Prediction of CYP2D6-Mediated Gene-Drug-Drug Interactions. Daali, Y; Desmeules, J; Storelli, F, 2019)	0.51

Excerpt	Reference	Relevance
" The bioavailability of dextromethorphan hydrobromide after 30 mg po, as measured by the concentration of total (free and conjugated) dextrorphan in the plasma, was determined in six human volunteers with this procedure."	( Determination of dextrorphan in plasma and evaluation of bioavailability of dextromethorphan hydrobromide in humans. Emele, JF; Ramachander, G; Williams, FD, 1977)	0.79
"9% compared with the intravenous route, whereas the plasma bioavailability from the nasal route was 78."	( Nasal delivery of [14C]dextromethorphan hydrochloride in rats: levels in plasma and brain. Behl, CR; Char, H; Iqbal, K; Kumar, S; Malick, AW; Patel, S; Piemontese, D; Salvador, RA, 1992)	0.59
"A large interindividual variability for clozapine bioavailability and plasma steady-state concentrations and clearance exists."	( The antipsychotic clozapine is metabolized by the polymorphic human microsomal and recombinant cytochrome P450 2D6. Fischer, V; Maurer, G; Tynes, RE; Vogels, B, 1992)	0.28
"We compared in this double-blind crossover study the bioavailability of dextromethorphan from a dextromethorphan-salbutamol combination tablet (Redol comp) and from a plain dextromethorphan tablet (Extuson) by determining dextrorphan concentrations after single-dose oral administration in 10 healthy volunteers."	( Pharmacokinetic comparison of a dextromethorphan-salbutamol combination tablet and a plain dextromethorphan tablet. Happonen, P; Karttunen, P; Mykkänen, M; Romppanen, T; Silvasti, M; Tukiainen, H, 1990)	0.79
"A randomized, two-way, steady-state crossover study was performed in 24 healthy male volunteers to evaluate the bioavailability of a controlled-release (CR) dextromethorphan (DM) suspension."	( Bioavailability evaluation of a controlled-release dextromethorphan liquid. Amsel, LP; Dennis, SR; Hinsvark, ON; Rotenberg, KS; Woodworth, JR, 1987)	0.72
" Bioavailability of dextromethorphan tablets was comparable to syrup."	( Dextromethorphan and codeine: comparison of plasma kinetics and antitussive effects. Aylward, M; Davies, DE; Leideman, T; Maddock, J; Protheroe, DA, 1984)	2.03
"A reverse-phase High Performance Liquid Chromatographic (HPLC) method was developed for the analysis of metoprolol in the large number of human plasma samples obtained in in vitro-in vivo correlations (IVIVC) and bioavailability studies of extended release formulations of metoprolol tartrate."	( A sensitive assay of metoprolol and its major metabolite alpha-hydroxy metoprolol in human plasma and determination of dextromethorphan and its metabolite dextrorphan in urine with high performance liquid chromatography and fluorometric detection. Eddington, NE; Leslie, J; Mistry, B, 1998)	0.51
"A multiple dose bioavailability study with six healthy male human volunteers was conducted."	( Bioavailability of dextromethorphan (as dextrorphan) from sustained release formulations in the presence of guaifenesin in human volunteers. Demirbas, S; Reyderman, L; Stavchansky, S, 1998)	0.63
" Bioavailability (F) of DM increased significantly with grapefruit and seville orange juice, but only returned to half the baseline value after three days of washout."	( The effect of grapefruit juice and seville orange juice on the pharmacokinetics of dextromethorphan: the role of gut CYP3A and P-glycoprotein. Di Marco, MP; Ducharme, MP; Edwards, DJ; Wainer, IW, 2002)	0.54
" Oral bioavailability was 11% as calculated from naive pooled data."	( Plasma profile and pharmacokinetics of dextromethorphan after intravenous and oral administration in healthy dogs. Kukanich, B; Papich, MG, 2004)	0.59
"The aim of this study was to compare the bioavailability of cyclosporine (CyA) from the generic dispersion formulation Cicloral (CIC) with the microemulsion formulation Neoral (NEO) and the original Sandimmune (SIM) capsules after single doses of 100, 300, or 600 mg of drug, respectively."	( Comparative bioavailability of the microemulsion formulation of cyclosporine (Neoral) with a generic dispersion formulation (Cicloral) in young healthy male volunteers. Bucher, M; Burhenne, J; Faerber, L; Gschaidmeier, H; Kees, F; Mikus, G; Schweda, F, 2006)	0.33
"To assess the single-dose absolute oral bioavailability of traxoprodil in healthy male volunteers phenotyped as either CYP2D6 extensive or poor metabolisers."	( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers. Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006)	0.33
"In poor metabolisers (n = 6), oral bioavailability was approximately 80% and was consistent with a liver extraction ratio of approximately 20% (plasma clearance of approximately 4 mL/min/kg) indicating near complete absorption."	( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers. Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006)	0.33
" In extensive metabolisers, the oral bioavailability was nonlinear and dose-dependent, while in poor metabolisers, oral bioavailability appeared to be linear and dose-independent."	( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers. Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006)	0.33
" DM's limited clinical benefit is proposed to be associated with its rapid metabolism to dextrorphan, which restricts its central bioavailability and therapeutic utility."	( Dextromethorphan as a potential neuroprotective agent with unique mechanisms of action. Calef, U; Lauterbach, EC; Werling, LL, 2007)	1.78
"The data support an alteration in bioavailability due to an AMD070-mediated inhibition of presystemic metabolism, though an intestinal P-glycoprotein effect could also be contributing."	( Pharmacokinetic effect of AMD070, an Oral CXCR4 antagonist, on CYP3A4 and CYP2D6 substrates midazolam and dextromethorphan in healthy volunteers. Becker, S; Calandra, GB; Chee, P; Everts, S; Hendrix, CW; MacFarland, RT; Nyunt, MM; Scarborough, R, 2008)	0.56
" A complete cross-over bioavailability study of the optimized formulation of the developed sustained tablets and marketed immediate release tablets was performed on six healthy male volunteers."	( Formulation and evaluation of dextromethorphan hydrobromide sustained release tablets. Krishnaraj, K; Meyyanathan, SN; Muralidaharan, S; Rajan, S; Siddaiah, MK; Suresh, B, 2008)	0.63
" DM has been under investigation for several years as a neuroprotective agent in stroke, neurosurgery and amyotrophic lateral sclerosis (ALS); however, it is rapidly metabolized by CYP2D6, reducing the drug's bioavailability at neuronal targets."	( AVP-923, a combination of dextromethorphan hydrobromide and quinidine sulfate for the treatment of pseudobulbar affect and neuropathic pain. Olney, N; Rosen, H, 2010)	0.66
"To establish an high-performance liquid chromatography (HPLC)-based method for analysis of the pharmacokinetics and relative bioavailability of dextromethorphan chewing gum tablets in rabbits."	( [Pharmacokinetic study of a new chewing gum dextromethorphan delivery system]. Liu, BL; Liu, J; Tan, QY; Xu, ML; Zhang, JQ; Zhao, CJ, 2011)	0.83
"The pharmacokinetic parameters and the relative bioavailability of dextromethorphan chewing gum preparation in rabbits were compared with those of the commercially available chewing dextromethorphan tablets using 3P97 software."	( [Pharmacokinetic study of a new chewing gum dextromethorphan delivery system]. Liu, BL; Liu, J; Tan, QY; Xu, ML; Zhang, JQ; Zhao, CJ, 2011)	0.87
" The relative bioavailability of the new chewing gum medicine system was (140."	( [Pharmacokinetic study of a new chewing gum dextromethorphan delivery system]. Liu, BL; Liu, J; Tan, QY; Xu, ML; Zhang, JQ; Zhao, CJ, 2011)	0.63
" However, maximum plasma concentration, half-life, area under the curve, and oral bioavailability were not different."	( Pharmacokinetic and pharmacodynamic alterations in the Roux-en-Y gastric bypass recipients. Chalasani, N; Hall, SD; Jones, DR; Mattar, S; Tandra, S; Vuppalanchi, R, 2013)	0.39
" Quinidine, a cytochrome P450 (CYP) 2D6 inhibitor, was also evaluated in conjunction with dextromethorphan to increase the bioavailability of dextromethorphan and reduce exposure to additional metabolites."	( Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan. Healy, JR; Matsumoto, RR; Nguyen, L; Robson, MJ; Scandinaro, AL, 2014)	0.86
" In the past few years, many studies showed that borneol can improve the bioavailability of other drugs, promoting drugs to cross the blood-brain barrier, so the potential drug interactions between borneol and other medicines have attracted great attention, but the influence of borneol to CYP450 and its isoforms are rarely reported."	( [Borneol is an inducer of rat hepatic CYP2D activity in vivo]. Chen, JY; Chen, Y; Meng, MR; Wang, JJ, 2015)	0.42
" Coadministration of DM with a low dose of quinidine inhibits DM metabolism, yields greater bioavailability and enables more specific testing of the therapeutic properties of DM apart from its metabolites."	( Pharmacology of dextromethorphan: Relevance to dextromethorphan/quinidine (Nuedexta®) clinical use. Matsumoto, RR; Pope, LE; Siffert, J; Taylor, CP; Traynelis, SF, 2016)	0.78
" This study shows that dissolution and the rate of absorption into the enterocytes are clinically irrelevant for the performance of DEX immediate release product."	( The Irrelevance of In Vitro Dissolution in Setting Product Specifications for Drugs Like Dextromethorphan That are Subject to Lysosomal Trapping. Almukainzi, M; Bolger, MB; Löbenberg, R; Macwan, JS; Sarfraz, M, 2019)	0.74
" However, the bioavailability of 3-HM is very low due to the rapid first-pass metabolism of the phenolic moiety."	( Design, Synthesis, and Biological Evaluation of Phenol Bioisosteric Analogues of 3-Hydroxymorphinan. Bai, X; Bao, X; Li, Z; Shang, J; Sheng, C; Wang, J; Wang, Y; Zhang, D; Zhang, G; Zhu, M, 2019)	0.51
"Common cold symptoms may be mitigated by products in caplet, nasal spray, and oral solution formulations, although variations exist in the bioavailability of the active ingredients contained within these products."	( A single-dose, open-label, randomized, scintigraphic study to investigate the gastrointestinal behavior of 2 triple-combination cold products (acetaminophen, phenylephrine, and dextromethorphan) in healthy male volunteers. Armogida, M; Doll, WJ; Mallefet, P; Page, RC; Sandefer, EP, 2022)	0.91

Excerpt	Relevance	Reference
" Therapy with benzoate, 500 mg/kg per day, was started on day 5, and the dosage was increased to 750 mg/kg per day on day 8, with prompt normalization of the neurologic and electroencephalographic findings."	( Dextromethorphan and high-dose benzoate therapy for nonketotic hyperglycinemia in an infant. Francomano, CA; Hamosh, A; Johnston, MV; McDonald, JW; Niedermeyer, E; Valle, D, 1992)	1.73
", the morphine dose-response curve was shifted to the right."	( Potentiation of disruptive effects of dextromethorphan by naloxone on fixed-interval performance in rats. Taşkin, T, 1986)	0.54
" Blood samples were collected over a 12-hour dosing period on the last day of each treatment and analyzed for DM and its active metabolite, dextrorphan (DP)."	( Bioavailability evaluation of a controlled-release dextromethorphan liquid. Amsel, LP; Dennis, SR; Hinsvark, ON; Rotenberg, KS; Woodworth, JR, 1987)	0.52
"A high-performance liquid chromatographic (HPLC) method has been developed for the quantitation of acetaminophen, chlorpheniramine maleate, dextromethorphan hydrobromide, and phenylpropanolamine hydrochloride in combination in pharmaceutical dosage forms using a single column and three different mobile phases."	( Quantitation of acetaminophen, chlorpheniramine maleate, dextromethorphan hydrobromide, and phenylpropanolamine hydrochloride in combination using high-performance liquid chromatography. Das Gupta, V; Heble, AR, 1984)	0.71
"Plasma kinetics of dextromethorphan (as dextrorphan ) and codeine were investigated after acute oral doses in 8 patients with pathological cough; after which the patients participated in an acute dose-response study of the antitussive effects of each drug administered as syrups."	( Dextromethorphan and codeine: comparison of plasma kinetics and antitussive effects. Aylward, M; Davies, DE; Leideman, T; Maddock, J; Protheroe, DA, 1984)	2.04
"8 years), all urine EMIT assays six hours after ingestion of dextromethorphan, at both dosage levels, were negative for opioids and all other drugs."	( The dextromethorphan defense: dextromethorphan and the opioid screen. Magoon, MR; Norton, J; Storrow, AB, 1995)	1.09
" Interpopulation differences in the prevalence of deficiencies of drug-metabolizing enzymes may be clinically important in the selection and dosage of drug therapies for patients."	( Comparison of the prevalence of the poor metabolizer phenotype for CYP2D6 between 203 Hmong subjects and 280 white subjects residing in Minnesota. Hansen, SR; Straka, RJ; Walker, PF, 1995)	0.29
"Tolerance to the antinociceptive (analgesic) effect of morphine, a mu-opioid agonist, was developed in male CD-1 mice as assessed by a shift to the right of the analgesic (tail-flick) dose-response curves and an increase in the ED50 values."	( Dextromethorphan attenuates and reverses analgesic tolerance to morphine. Elliott, K; Hynansky, A; Inturrisi, CE, 1994)	1.73
"0 nm, respectively, have been developed for the specific determination of guaiphenesin in the presence of dextromethorphan, drugs with closely overlapping absorption spectra, in synthetic admixtures and in pharmaceutical dosage forms (tablets and syrups)."	( Determination of guaiphenesin in anti-tussive pharmaceutical preparations containing dextromethorphan by first- and second-derivative ultraviolet spectrophotometry. Hu, TM; Lee, AR, 1994)	0.73
" In many instances, a knowledge of the drug metabolism status of a patient can be helpful in the selection of a drug and its dosage regimen, and in the prediction of possible drug/drug interactions when two or more drugs have to be administered concomitantly."	( Polymorphism in the metabolism of drugs, including antidepressant drugs: comments on phenotyping. Coutts, RT, 1994)	0.29
" Concentrations in plasma were determined after 7 days of desipramine (50 mg/day) dosing alone, during the 21 days of desipramine and selective serotonin reuptake inhibitor (SSRI) coadministration (fluoxetine, 20 mg/day; sertraline, 50 mg/day), and for 21 days of continued desipramine administration after SSRI discontinuation."	( Pharmacokinetics of desipramine coadministered with sertraline or fluoxetine. Alderman, J; Chung, M; Harris, S; Harrison, W; Messig, M; Preskorn, SH, 1994)	0.29
" Patients were sequentially dosed with DM 40 mg/6 h (8 weeks) and 50 mg/6 h (8 weeks) while concurrent antiepileptic drugs were kept stable."	( Pharmacokinetics of dextromethorphan and dextrorphan in epileptic patients. Kazis, A; Kimiskidis, V; Niopas, I, )	0.45
" Serial plasma and urine samples were collected at specified time intervals after dosing on Days 1, 16, 18, 20 and 22."	( Single and multiple dose pharmacokinetics of nefazodone in subjects classified as extensive and poor metabolizers of dextromethorphan. Barbhaiya, RH; Buch, AB; Greene, DS, 1996)	0.5
"After CYP2D6 phenotype determination with dextromethorphan, 31 patients were treated with oral DMI at a dosage of 100 mg per day for 3 weeks."	( Relationship between plasma desipramine levels, CYP2D6 phenotype and clinical response to desipramine: a prospective study. Avenoso, A; Campo, GM; Caputi, AP; Gitto, C; Perucca, E; Spina, E, 1997)	0.56
" The two patients with the poor metabolizer phenotype showed the highest plasma concentrations of DMI and complained of severe adverse effects, requiring dosage reduction."	( Relationship between plasma desipramine levels, CYP2D6 phenotype and clinical response to desipramine: a prospective study. Avenoso, A; Campo, GM; Caputi, AP; Gitto, C; Perucca, E; Spina, E, 1997)	0.3
" In the patient with the apparent poor metabolizer (PM) phenotype, a change in the DM preparation to a sustained-release form and increase in the dosing interval was required to lower DM plasma concentrations."	( Dextromethorphan in nonketotic hyperglycinaemia: metabolic variation confounds the dose-response relationship. Arnold, GL; Griebel, ML; Kearns, GL; Koroma, DM; Valentine, JL, 1997)	1.74
"3 mm3 (mean +/- standard error of the mean), while animals receiving dextromethorphan had significantly smaller lesions, which was independent of dosing schedule (59."	( Neuroprotection by dextromethorphan in acute experimental subdural hematoma in the rat. Boardman, C; Duhaime, AC; Gennarelli, LM, 1996)	0.86
" Dosage was titrated in each patient to the highest level reached without disrupting normal activities; mean doses were 381 mg/day in diabetics and 439 mg/day in postherpetic neuralgia patients."	( High-dose oral dextromethorphan versus placebo in painful diabetic neuropathy and postherpetic neuralgia. Max, MB; Nelson, KA; Park, KM; Robinovitz, E; Tsigos, C, 1997)	0.65
" IB showed a dose-response relationship which appeared to plateau at doses of 50 and 100 mg/kg."	( Effects of the combined oral administration of NSAIDs and dextromethorphan on behavioral symptoms indicative of arthritic pain in rats. Caruso, FS; Frenk, H; Lu, J; Mao, J; Mayer, DJ; Price, DD, 1996)	0.54
" Therefore the determination of dextromethorphan and metabolites in serum could be advantageous to measure individual CYP2D6 activities in vivo and thus optimize the dosing of drugs metabolized by CYP2D6."	( CYP2D6 genotype and phenotyping by determination of dextromethorphan and metabolites in serum of healthy controls and of patients under psychotropic medication. Fuchs, K; Härtter, S; Hiemke, C; Köhler, D; Sieghart, W, 1997)	0.83
" The dosage of sertraline ranged from 25 to 150 mg/day (93."	( The extent and determinants of changes in CYP2D6 and CYP1A2 activities with therapeutic doses of sertraline. Herrmann, N; Kalow, W; Naranjo, CA; Ozdemir, V; Reed, K; Sellers, EM; Shulman, RW, 1998)	0.3
"03 mg/kg/infusion), suggesting that DM shifted the dose-response curve for cocaine self-administration to the left."	( Dextromethorphan alters the reinforcing effect of cocaine in the rat. Hong, SY; Jhoo, WK; Kim, HC; Park, BK, 1997)	1.74
" Levodopa dose-response curves for antiparkinsonian and dyskinetic effects were then compared for each study arm."	( Dextromethorphan improves levodopa-induced dyskinesias in Parkinson's disease. Chase, TN; Del Dotto, P; Natté, R; van den Munckhof, P; Verhagen Metman, L, 1998)	1.74
"Intravenous and oral verapamil clearance values were significantly correlated, and cumulative dextromethorphan/3-methoxymorphinan urinary ratios correlated with both plasma AUC(norverapamil)/AUC(verapamil) after oral verapamil dosing and with oral and intravenous verapamil clearance."	( In vivo comparison of putative probes of CYP3A4/5 activity: erythromycin, dextromethorphan, and verapamil. Barnas, CR; Gorski, JC; Krecic-Shepard, ME; Schwartz, JB; Slimko, J; Wainer, IW, 1999)	0.75
" We compared metabolic ratios from six different dextromethorphan phenotyping doses to ascertain whether linearity existed over a dosage range."	( Dose dependency of dextromethorphan for cytochrome P450 2D6 (CYP2D6) phenotyping. Bertino, JS; Ellis, RE; Gaedigk, A; Gotschall, R; Kearns, GL; Leeder, JS; Nafziger, AN; Streetman, DS, 1999)	0.89
"9-fold rightward shift of the cumulative dose-response curves."	( Clinically available NMDA receptor antagonists memantine and dextromethorphan reverse existing tolerance to the antinociceptive effects of morphine in mice. Danysz, W; Kozela, E; Popik, P, 2000)	0.55
"A high performance liquid chromatography procedure has been developed for the simultaneous determination of guaifenesin pseudoephedrine-dextromethorphan and guaifenesin-pseudoephedrine in commercially available capsule dosage forms and guaifenesin-codeine in a commercial cough syrup dosage form."	( HPLC determination of guaifenesin with selected medications on underivatized silica with an aqueous-organic mobile phase. Stewart, JT; Wilcox, ML, 2000)	0.51
" Dosage was titrated in each patient to the highest level reached without disrupting normal activities."	( A randomized, controlled trial of high-dose dextromethorphan in facial neuralgias. Booher, SL; Gilron, I; Max, MB; Rowan, MS; Smoller, MS, 2000)	0.57
" Knowledge of the percolation threshold -- one of the most important concepts in percolation theory -- results in a clear improvement of the solid dosage form design."	( Estimation of the percolation thresholds in dextromethorphan hydrobromide matrices. Caraballo, I; Melgoza, LM; Rabasco, AM; Sandoval, H, 2001)	0.57
"The inhibition potential of drugs towards five major human hepatic cytochrome P450 (CYP) isozymes (CYP2A6, 3A4, 2C9, 2D6, and 2E1) was investigated via cassette dosing of the five probe substrates (coumarin, midazolam, tolbutamide, dextromethorphan, and chlorzoxazone) in human liver microsomes using a 96-well plate format."	( High-throughput cytochrome P450 (CYP) inhibition screening via a cassette probe-dosing strategy. VI. Simultaneous evaluation of inhibition potential of drugs on human hepatic isozymes CYP2A6, 3A4, 2C9, 2D6 and 2E1. Bu, HZ; Knuth, K; Magis, L; Teitelbaum, P, 2001)	0.49
" Three days of validation data are provided along with study sample data from a patient dosed with commercially available Vicks 44."	( Increasing bioanalytical throughput using pcSFC-MS/MS: 10 minutes per 96-well plate. Bolden, RD; Hoke, SH; Morand, KL; Pinkston, JD; Tomlinson, JA; Wehmeyer, KR, 2001)	0.31
" Tolbutamide (CYP2C9), caffeine (CYP1A2), dextromethorphan (CYP2D6), oral midazolam (intestinal wall and hepatic CYP3A), and intravenous midazolam (hepatic CYP3A) were administered before, with short-term St John's wort dosing (900 mg), and after 2 weeks of intake (300 mg 3 times a day) to determine CYP activities."	( The effects of St John's wort (Hypericum perforatum) on human cytochrome P450 activity. Gorski, JC; Hall, SD; Hamman, MA; Huang, SM; Lesko, LJ; Wang, Z, 2001)	0.57
" active placebo [lorazepam]) and (2) dose-response trial of the preferred active drug in responders from the first study (0% vs."	( Dextromethorphan and memantine in painful diabetic neuropathy and postherpetic neuralgia: efficacy and dose-response trials. Booher, S; Gilron, I; Max, MB; Parada, S; Sang, CN, 2002)	1.76
" Blood pressure and heart rate were also monitored before dosing and after the dosing regimen."	( Assessment of the effect of dextromethorphan and ketamine on the acute nociceptive threshold and wind-up of the second pain response in healthy male volunteers. Fisher, G; Growcott, JW; Hughes, AM; Rhodes, J; Sellers, M, 2002)	0.61
"For paroxetine and fluoxetine, plasma concentrations and dosage strongly influence the magnitude of enzyme inhibition."	( CYP2D6 inhibition by selective serotonin reuptake inhibitors: analysis of achievable steady-state plasma concentrations and the effect of ultrarapid metabolism at CYP2D6. Alfaro, CL; Ereshefsky, L; Gaedigk, A; Lam, YW; Simpson, J, 2002)	0.31
"Oral dextromethorphan (120-180 mg daily) was administered to three selected cancer patients during a 3-week study and an additional 1 month of treatment with the dosage subjectively judged to be best."	( Dextromethorphan for phantom pain attenuation in cancer amputees: a double-blind crossover trial involving three patients. Ben Abraham, R; Kollender, Y; Marouani, N; Meller, I; Weinbroum, AA, )	2.09
"Further clinical trials are warranted to determine the optimal dosage and identify which patients with phantom pain would benefit the most from this therapeutic approach."	( Dextromethorphan for phantom pain attenuation in cancer amputees: a double-blind crossover trial involving three patients. Ben Abraham, R; Kollender, Y; Marouani, N; Meller, I; Weinbroum, AA, )	1.57
" Using a mouse hot-plate test, dose-response relationships were first determined for all compounds individually and then for opioids co-administered with fixed doses of ketamine or dextromethorphan."	( Dextromethorphan and ketamine potentiate the antinociceptive effects of mu- but not delta- or kappa-opioid agonists in a mouse model of acute pain. Baker, AK; Hoffmann, VL; Meert, TF, 2002)	1.95
" Using a mouse hot-plate test, dose-response relationships were first determined for all compounds individually and then for opioids co-administered with fixed doses of clonidine, ketamine or dextromethorphan."	( Interactions of NMDA antagonists and an alpha 2 agonist with mu, delta and kappa opioids in an acute nociception assay. Baker, AK; Hoffmann, VL; Meert, TF, 2002)	0.5
"In this study, the metabolic ratios of dextromethorphan to dextrorphan (DM/DX) in plasma were calculated at steady state after administering 2 dosage forms (Medicon) and Detusiv) of DM with different release rates."	( Analysis of pharmacokinetic parameters for assessment of dextromethorphan metabolic phenotypes. Chen, JY; Ho, HO; Lee, YJ; Sheu, MT; Tao, PL; Yeh, GC, )	0.65
" After 14 days of St John's wort administration, participants were given the probe drugs along with 1 St John's wort tablet to establish postadministration CYP activity; the St John's wort dosing regimen was continued for 48 hours."	( Effect of St John's wort on drug metabolism by induction of cytochrome P450 3A4 enzyme. Chavin, KD; DeVane, CL; Donovan, JL; Markowitz, JS; Ruan, Y; Taylor, RM; Wang, JS, 2003)	0.32
" This suggests that long-term administration of St John's wort may result in diminished clinical effectiveness or increased dosage requirements for all CYP 3A4 substrates, which represent at least 50% of all marketed medications."	( Effect of St John's wort on drug metabolism by induction of cytochrome P450 3A4 enzyme. Chavin, KD; DeVane, CL; Donovan, JL; Markowitz, JS; Ruan, Y; Taylor, RM; Wang, JS, 2003)	0.32
" Naloxone, which had no effect on the dextromethorphan dose-response relation, abolished the synergism."	( Morphine potentiates dextromethorphan-induced vasodilation in rat superior mesenteric artery. Inan, S; Tallarida, RJ, 2004)	0.91
"The aim of this work was to determine whether a dose-response relationship existed among a group of children administered a single nocturnal dose of DM for cough due to an upper respiratory tract infection."	( Dose-response relationship with increasing doses of dextromethorphan for children with cough. Baker, MS; Berlin, CM; Paul, IM; Shaffer, ML; Sturgis, SA; Yoder, KE, 2004)	0.57
" The direction of dosing adjustments during pregnancy will depend on the drug and the enzyme that is responsible for its metabolism."	( Temporal changes in drug metabolism (CYP1A2, CYP2D6 and CYP3A Activity) during pregnancy. Caritis, SN; Glover, DD; Tracy, TS; Venkataramanan, R, 2005)	0.33
"Twenty-eight randomized, double-blind, clinical studies, with 40 comparisons, including a variety of dosing regimens comparing DM treatment with placebo, were included."	( A qualitative systematic review of peri-operative dextromethorphan in post-operative pain. Dahl, JB; Duedahl, TH; Møiniche, S; Rømsing, J, 2006)	0.59
" Subsequently blood and urine samples were collected after drug dosing as before."	( Effect of honey on CYP3A4, CYP2D6 and CYP2C19 enzyme activity in healthy human volunteers. Adithan, C; Rajan, S; Shashindran, C; Tushar, T; Vinod, T, 2007)	0.34
" The objective measure of cough reflex sensitivity was the citric acid, dose-response cough challenge."	( Assessment of antitussive efficacy of dextromethorphan in smoking related cough: objective vs. subjective measures. Hull, D; Morice, AH; Ramsay, J; Thompson, R; Wright, C, 2008)	0.62
" The risk of overdose, incorrect dosing and adverse events is increased in young children due to the greater number of colds they acquire each year."	( Over-the-counter cough and cold medication use in young children. Brewer, M; Ryan, T; Small, L, )	0.13
" In vivo assessment of CYP1A2 and CYP3A4 activities, perhaps by phenotyping approaches, could assist the optimization of CLZ dosage and minimize pharmacokinetic interactions with coadministered drugs."	( Interindividual variation in relative CYP1A2/3A4 phenotype influences susceptibility of clozapine oxidation to cytochrome P450-specific inhibition in human hepatic microsomes. D'Esposito, F; Edwards, RJ; Murray, M; Ramzan, I; Zhang, WV, 2008)	0.35
" Arterial rings were mounted in isolated tissue chambers equipped with isometric tension transducers to obtain pharmacologic dose-response curves."	( N-methyl-D-aspartate (NMDA) antagonists--S(+)-ketamine, dextrorphan, and dextromethorphan--act as calcium antagonists on bovine cerebral arteries. Carlsson, C; Chen, D; Harakal, C; Kamel, IR; Wendling, KS; Wendling, WW, 2008)	0.58
"0 x 10(-3) M DXM hydrobromide in pure as well as in dosage forms by direct potentiometry and standard addition methods."	( Polymeric membrane sensors for the selective determination of dextromethorphan in pharmaceutical preparations. El-Naby, EH, 2008)	0.59
" Information on a respective dose-response relationship is not available."	( Dose-response relationship for the pharmacokinetic interaction of grapefruit juice with dextromethorphan investigated by human urinary metabolite profiles. Bittner, N; Lutz, U; Lutz, WK; Strauch, K, 2009)	0.58
" In an acute (3 day) dose-response study, anesthetized male Sprague-Dawley rats were exposed to a unilateral frontal PBBI with DM (0."	( Neuroprotective profile of dextromethorphan in an experimental model of penetrating ballistic-like brain injury. Lu, XC; Sharrow, K; Shear, DA; Tortella, FC; Williams, AJ, 2009)	0.65
" After cerebral infarction, intravenous dosing of saline had no effect on these parameters."	( Ameliorating effects of cloperastine on dysfunction of the urinary bladder caused by cerebral infarction in conscious rats. Shirasaki, T; Soeda, F; Takahama, K; Yamamoto, G, 2009)	0.35
"Compared to the no quinidine condition, quinidine pre-treatment decreased the area under the dose-response curve on subjective measures of positively reinforcing effects (e."	( Effect of metabolic blockade on the psychoactive effects of dextromethorphan. Busto, U; Sellers, EM; Tyndale, RF; Zawertailo, LA, 2010)	0.6
" Of particular concern to the FDA were increased QTc intervals reported in patients dosed with a 30-/30-mg dose of DM/Q."	( AVP-923, a combination of dextromethorphan hydrobromide and quinidine sulfate for the treatment of pseudobulbar affect and neuropathic pain. Olney, N; Rosen, H, 2010)	0.66
" Other endpoints showing statistically significant DMq benefit included, for both dosage levels, the likelihood of PBA remission during the final 14 days and, for the higher dosage, improvement on measures of social functioning and mental health."	( Dextromethorphan plus ultra low-dose quinidine reduces pseudobulbar affect. Brooks, BR; Cummings, J; Hepner, A; Kaye, R; Pioro, EP; Schiffer, R; Thisted, RA; Wynn, D, 2010)	1.8
"First, dose-response curves for dextromethorphan, dextrorphan, and bupivacaine (n = 8 at each testing point) were determined for cutaneous analgesia on the rat back, and equipotent doses were calculated."	( Systemic dextromethorphan and dextrorphan are less toxic in rats than bupivacaine at equianesthetic doses. Chen, YC; Chen, YW; Hung, CH; Liu, TY; Wang, JJ, 2011)	1.07
" This test could contribute to the personalization and optimization of tamoxifen treatment, but it needs additional validation and simplification before being applicable in future dosing strategies."	( Dextromethorphan as a phenotyping test to predict endoxifen exposure in patients on tamoxifen treatment. Beijnen, JH; de Graan, AJ; de Jongh, FE; de Vos, AI; de Vos, FY; Loos, WJ; Mathijssen, RH; Seynaeve, C; Teunissen, SF; van Alphen, RJ; van der Holt, B; van Schaik, RH; Verweij, J, 2011)	1.81
" The approved dosage of DMQ is DM 20 mg and Q 10 mg twice daily."	( Randomized open-label drug-drug interaction trial of dextromethorphan/quinidine and paroxetine in healthy volunteers. Pope, LE; Schoedel, KA; Sellers, EM, 2012)	0.63
" Thus, patients should be monitored for AEs and dosage adjustment considered when combining these two agents."	( Randomized open-label drug-drug interaction trial of dextromethorphan/quinidine and paroxetine in healthy volunteers. Pope, LE; Schoedel, KA; Sellers, EM, 2012)	0.63
" Concomitant use of drugs metabolized by CYP2D6 may require dosage adjustment."	( Pharmacokinetic drug interactions between clobazam and drugs metabolized by cytochrome P450 isoenzymes. Bekersky, I; Blum, RA; Tolbert, D; Walzer, M, 2012)	0.38
"Orally disintegrating tablets (ODTs), which disintegrate rapidly (<1 min) in the mouth and do not require water for administration, have become a very popular dosage form."	( Development and optimization of dextromethorphan hydrobromide oral disintegrating tablets: effect of formulation and process variables. Ibrahim, MA; Mostafa, HF; Sakr, A, )	0.41
" Therefore, we asked if a physiologically based pharmacokinetic (PBPK) model could be used to evaluate different dosing regimens for pregnant women."	( A physiologically based pharmacokinetic model to predict disposition of CYP2D6 and CYP1A2 metabolized drugs in pregnant women. Isoherranen, N; Ke, AB; Nallani, SC; Rostami-Hodjegan, A; Unadkat, JD; Zhao, P, 2013)	0.39
" However, a higher dosage of DXM antagonized the differentiation of osteoblasts via the inhibition of osteogenic signals and increase of adipogenic signals."	( Dextromethorphan inhibits osteoclast differentiation by suppressing RANKL-induced nuclear factor-κB activation. Chen, YR; Fu, WM; Lin, TH; Liou, HC; Lu, DH; Wu, K; Yang, RS, 2013)	1.83
" The former, on sale without prescription, presents a varied symptomatology, dosage and dependent metabolic action, ranging from euphoria to hallucinations."	( [Emergent drugs (II): the Pharming phenomenon]. Aldea-Perona, A; Burillo-Putze, G; Climent, B; Dueñas, A; García-Sáiz, MM; Hoffman, RS; Munné, P; Nogué, S; Rodríguez-Jiménez, C, )	0.13
" However, C-10068 failed to improve PBBI-induced motor and cognitive functions with the dosing regimen used in this study."	( Dual Therapeutic Effects of C-10068, a Dextromethorphan Derivative, Against Post-Traumatic Nonconvulsive Seizures and Neuroinflammation in a Rat Model of Penetrating Ballistic-Like Brain Injury. Bridson, GW; Chen, Z; Graham, PB; Leung, LY; Lu, XC; Shear, DA; Tortella, FC; Uttamsingh, V, 2015)	0.69
" NIC abolished anodal tDCS-induced motor cortex excitability enhancement, which was restituted under medium dosage of DMO."	( Mechanisms of Nicotinic Modulation of Glutamatergic Neuroplasticity in Humans. Batsikadze, G; Fresnoza, S; Grundey, J; Kuo, MF; Lugon, MDMV; Nakamura-Palacios, EM; Nitsche, MA; Paulus, W, 2017)	0.46
" The outcome on developmental progress and seizures was compared between the first child diagnosed and treated late with the second child diagnosed at birth and treated aggressively from the newborn period using dextromethorphan and benzoate at dosing sufficient to normalize plasma glycine levels."	( Neurodevelopmental Outcome and Treatment Efficacy of Benzoate and Dextromethorphan in Siblings with Attenuated Nonketotic Hyperglycinemia. Ahmad, A; Bjoraker, KJ; Burns, C; Christodoulou, J; Coughlin, CR; Creadon-Swindell, G; Dyack, S; Fergeson, M; Friederich, MW; Gaughan, S; Hodge, MA; Spector, EB; Swanson, MA; Tan, ES; Van Hove, JL, 2016)	0.86
" However, the optimal dose and safety of chronic dosing are not fully known."	( Dextromethorphan: An update on its utility for neurological and neuropsychiatric disorders. Cavendish, JZ; Crowe, MS; Lucke-Wold, BP; Matsumoto, RR; Nguyen, L; Thomas, KL, 2016)	1.88
" Metabolic ratios (MRs) from AUC∞ after single dosing and from AUC0-12h at steady state were taken as the gold standard."	( Alternative methods for CYP2D6 phenotyping: comparison of dextromethorphan metabolic ratios from AUC, single point plasma, and urine. Chen, R; Hu, P; Shi, J; Wang, H, 2016)	0.68
" Present investigation was carried out in rats to study influence of corticosteroids after repeated dosing with/without pre-treatment with CYP2D inhibitor quinidine on the CYP2D1 mRNA levels and CYP2D enzyme activity using dextromethorphan as probe substrate."	( Consequences of daily corticosteroid dosing with or without pre-treatment with quinidine on the in vivo cytochrome P450 2D (CYP2D) enzyme in rats: effect on O-demethylation activity of dextromethorphan and expression levels of CYP2D1 mRNA. Delvadia, P; Giri, P; Gupta, L; Lad, K; Patel, HM; Patel, N; Srinivas, NR; Trivedi, P, 2018)	0.86
" High dosage of DXM can induce euphoria, dissociative effects and even hallucinations."	( Protective effect of Lycium Barbarum polysaccharides on dextromethorphan-induced mood impairment and neurogenesis suppression. Chan, JN; Fung, TK; Lau, BW; Leung, JW; Po, KK; Sánchez-Vidaña, DI; Sin, EL; Siu, AM; So, KF, 2017)	0.7
" Following dosing and euthanasia, rats decomposed outdoors to skeleton in two different microclimate environments (n = 5 ACU and n = 5 REP at each site): Site A (shaded forest microenvironment) and Site B (rocky substrate exposed to direct sunlight, 600 m from Site A)."	( Analysis of Dextromethorphan and Dextrorphan in Skeletal Remains Following Differential Microclimate Exposure: Comparison of Acute vs. Repeated Drug Exposure. Morrison, LM; Unger, KA; Watterson, JH, 2017)	0.83
"To evaluate the capacity for modafinil to be a perpetrator of metabolic drug-drug interactions by altering cytochrome P450 activity following a single dose and dosing to steady state."	( Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol. Mangoni, AA; Rowland, A; Sorich, MJ; van Dyk, M; Warncken, D, 2018)	0.48
"These data support consideration of the risk of clinically relevant metabolic drug-drug interactions perpetrated by modafinil when this drug is co-administered with drugs that are primarily cleared by CYP2C19 (single modafinil dose or steady state modafinil dosing) or CYP3A4 (steady state modafinil dosing only) catalysed metabolic pathways."	( Evaluation of modafinil as a perpetrator of metabolic drug-drug interactions using a model informed cocktail reaction phenotyping trial protocol. Mangoni, AA; Rowland, A; Sorich, MJ; van Dyk, M; Warncken, D, 2018)	0.48
" The in vitro data predicted ~ 50% decrease in CYP2D6 activity in humans after dosing with 13cisRA."	( Does In Vitro Cytochrome P450 Downregulation Translate to In Vivo Drug-Drug Interactions? Preclinical and Clinical Studies With 13-cis-Retinoic Acid. Amory, JK; Hogarth, C; Isoherranen, N; Kenny, JR; Kosaka, M; Stevison, F; Wong, S, 2019)	0.51
" He reported a subjective need to increase his dosing over time to achieve the same degree of intoxication."	( Ten Years of Robotripping: Evidence of Tolerance to Dextromethorphan Hydrobromide in a Long-Term User. Boley, SP; LeRoy, JM; Olives, TD; Stellpflug, SJ, 2019)	0.76
" The population-based human study analyzed the data from the Taiwan Longitudinal Health Insurance Database 2005 between January 2005 and December 2013 and then used the DXM dose-response curve to investigate the trend of its protective effect against PD."	( The effect of dextromethorphan use in Parkinson's disease: A 6-hydroxydopamine rat model and population-based study. Cheng, CY; Chien, WC; Chiu, CH; Huang, YS; Kao, LT; Li, IH; Liu, CT; Ma, KH; Shih, JH; Shiue, CY, 2019)	0.87
"Ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QToF-MS) analysis of dextromethorphan (DXM) and its metabolites-dextrorphan, 3-methoxymorphinan (3-MEM) and 3-hydroxymorphinan-in skeletal remains of rats exposed to DXM under different dosing patterns is described."	( Analysis of Dextromethorphan and Three Metabolites in Decomposed Skeletal Tissues by UPLC-QToF-MS: Comparison of Acute and Repeated Drug Exposures. Cornthwaite, HM; McDonald, CS; Watterson, JH, 2019)	1.1
" Diphenhydramine and dextromethorphan dosing errors were the most common cause of medication errors resulting from CCM use."	( Medication Errors From Over-the-Counter Cough and Cold Medications in Children. Banner, W; Bond, GR; Dart, RC; Green, JL; Kauffman, RE; Palmer, RB; Paul, IM; Rapp-Olsson, M; Reynolds, KM; Wang, GS, 2020)	0.88
" Blood samples were collected 3 h after dosing and plasma separated."	( Cytochrome P Chatterjee, S; Dhuya, M; Gogtay, N; Hazra, A; Pal, MM, )	0.13
" Incorporation of genotype-based dosing guidelines should be considered for CYP2D6 substrates given the prevalent use of these agents in this pediatric age group."	( A longitudinal study of cytochrome P450 2D6 (CYP2D6) activity during adolescence. Gaedigk, A; Leeder, JS; Lin, YS; Pearce, RE; Soden, SE; Staggs, VS; Wright, KJ, 2022)	0.72
"This study has a number of strengths including adequate power, a randomized controlled design, and an evidence-based dosing schedule."	( A double-blinded, placebo-controlled, randomized study to evaluate the efficacy of perioperative dextromethorphan compared to placebo for the treatment of postoperative pain: a study protocol. Christ, AB; Gilbert, PK; Gucev, GV; Heckmann, ND; Jones, IA; Lieberman, JR; Longjohn, DB; Oakes, DA; Piple, AS; Ratto, CE; Yan, PY, 2023)	1.13
" Eligible subjects met entry criteria and qualified by completing a run-in period where coughs were recorded with a cough monitor after they were dosed with sweet syrup."	( Objective and self-reported evidence of dextromethorphan antitussive efficacy in children, aged 6-11 years, with acute cough due to the common cold. Cruz-Rivera, M; Gelotte, CK; Jayawardena, S; Leyva, RA; Meeves, SG; Moreira, SA; Wilson, BL, 2023)	1.18

Role	Description
NMDA receptor antagonist	Any substance that inhibits the action of N-methyl-D-aspartate (NMDA) receptors. They tend to induce a state known as dissociative anesthesia, marked by catalepsy, amnesia, and analgesia, while side effects can include hallucinations, nightmares, and confusion. Due to their psychotomimetic effects, many NMDA receptor antagonists are used as recreational drugs.
neurotoxin	A poison that interferes with the functions of the nervous system.
xenobiotic	A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
environmental contaminant	Any minor or unwanted substance introduced into the environment that can have undesired effects.
antitussive	An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.
prodrug	A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
oneirogen	Any substance that produces or enhances dream-like states of consciousness.
[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
6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene	An organic heterotetracyclic compound that is 1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene which is substituted by a methoxy group at position 6 and a methyl group at position 11.
[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]

Pathway	Proteins	Compounds
Metabolism	1496	1108
Biological oxidations	150	276
Phase I - Functionalization of compounds	69	175
Cytochrome P450 - arranged by substrate type	30	110
Xenobiotics	4	50
Disease	1278	231
Infectious disease	895	79
SARS-CoV Infections	282	29
Potential therapeutics for SARS	59	2
Viral Infection Pathways	727	39

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	0.0063	0.0013	18.0743	39.8107	AID926; AID938
cytochrome P450 2D6 isoform 1	Homo sapiens (human)	Potency	2.5119	0.0020	7.5337	39.8107	AID891
muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Potency	10.8820	0.0010	6.0009	35.4813	AID943; AID944
[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)
Solute carrier family 22 member 1	Homo sapiens (human)	IC50 (µMol)	12.7250	0.2100	5.5537	10.0000	AID1442001; AID1526751
Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)	Ki	1.6800	0.0012	0.7025	6.0000	AID156805
Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)	Ki	1.6800	0.0012	0.7025	6.0000	AID156805
Neuronal acetylcholine receptor subunit alpha-3	Rattus norvegicus (Norway rat)	IC50 (µMol)	11.0500	0.0030	0.7770	6.0000	AID1174934
Sodium channel protein type 1 subunit alpha	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.6500	0.0100	1.1405	2.9390	AID179553; AID205275
Sodium channel protein type 2 subunit alpha	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.6500	0.0040	1.1485	4.7300	AID179553; AID205275
Sodium channel protein type 3 subunit alpha	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.6500	0.0060	0.8605	2.9390	AID179553; AID205275
Cytochrome P450 2D26	Rattus norvegicus (Norway rat)	IC50 (µMol)	5.6000	0.0940	2.1628	5.6000	AID54564
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	2.1768	0.0000	2.0151	10.0000	AID1862576; AID1884504; AID262947; AID54564; AID54570
Muscarinic acetylcholine receptor M2	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0001	0.5890	8.2600	AID142870
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	50.0000	0.0000	2.8005	10.0000	AID1210069
Neuronal acetylcholine receptor subunit beta-4	Rattus norvegicus (Norway rat)	IC50 (µMol)	11.0500	0.0030	0.8869	6.0000	AID1174934
Sodium-dependent serotonin transporter	Homo sapiens (human)	IC50 (µMol)	0.0027	0.0001	0.8645	8.7096	AID625222
Sodium-dependent serotonin transporter	Homo sapiens (human)	Ki	0.0014	0.0000	0.7048	8.1930	AID625222
Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)	Ki	2.2460	0.0003	0.8666	6.6900	AID157456
Cytochrome P450 2J2	Homo sapiens (human)	IC50 (µMol)	50.0000	0.0120	2.5312	9.4700	AID1210069
Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)	Ki	2.2460	0.0003	0.6805	6.6900	AID157456
Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)	Ki	2.2460	0.0003	0.7071	6.6900	AID157456
Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)	Ki	2.2460	0.0003	0.8196	6.6900	AID157456
Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)	Ki	1.6800	0.0012	0.4824	6.0000	AID156805
Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)	Ki	1.6800	0.0012	0.6205	6.0000	AID156805
Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)	Ki	1.6800	0.0012	0.3268	6.0000	AID156805
Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)	Ki	1.6800	0.0012	0.7025	6.0000	AID156805
Sigma non-opioid intracellular receptor 1	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.1236	0.0020	2.1233	10.0000	AID317399; AID317400
Sigma non-opioid intracellular receptor 1	Cavia porcellus (domestic guinea pig)	Ki	0.0365	0.0000	0.3385	10.0000	AID1744232; AID1744242
Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)	Ki	2.2460	0.0003	0.7072	6.6900	AID157456
Cytochrome P450 2D4	Rattus norvegicus (Norway rat)	IC50 (µMol)	136.0000	1.7000	1.7000	1.7000	AID54566
Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)	Ki	1.6800	0.0012	0.7025	6.0000	AID156805
Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)	Ki	2.2460	0.0003	0.7072	6.6900	AID157456
Sigma non-opioid intracellular receptor 1	Homo sapiens (human)	Ki	0.3480	0.0000	0.4901	10.0000	AID204634
Sigma non-opioid intracellular receptor 1	Rattus norvegicus (Norway rat)	Ki	5.0700	0.0003	0.2671	5.0700	AID203818
Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)	Ki	2.2460	0.0003	0.7072	6.6900	AID157456
[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)
Taste receptor type 2 member 46	Homo sapiens (human)	EC50 (µMol)	31.0000	0.0049	3.0983	8.6000	AID1622651
[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)
Cytochrome P450 2D6	Homo sapiens (human)	Km	1.4000	1.1000	3.7286	8.2000	AID1209237
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	Solute carrier family 22 member 1	Homo sapiens (human)
neurotransmitter transport	Solute carrier family 22 member 1	Homo sapiens (human)
serotonin transport	Solute carrier family 22 member 1	Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradient	Solute carrier family 22 member 1	Homo sapiens (human)
organic cation transport	Solute carrier family 22 member 1	Homo sapiens (human)
quaternary ammonium group transport	Solute carrier family 22 member 1	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 1	Homo sapiens (human)
monoamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
putrescine transport	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transport	Solute carrier family 22 member 1	Homo sapiens (human)
acetylcholine transport	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine transport	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 1	Homo sapiens (human)
epinephrine transport	Solute carrier family 22 member 1	Homo sapiens (human)
serotonin uptake	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine uptake	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
metanephric proximal tubule development	Solute carrier family 22 member 1	Homo sapiens (human)
purine-containing compound transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine uptake	Solute carrier family 22 member 1	Homo sapiens (human)
monoatomic cation transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
transport across blood-brain barrier	Solute carrier family 22 member 1	Homo sapiens (human)
(R)-carnitine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
acyl carnitine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
cellular detoxification	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Solute carrier family 22 member 1	Homo sapiens (human)
startle response	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
brain development	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
adult locomotory behavior	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
calcium-mediated signaling	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of synaptic plasticity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of neuronal synaptic plasticity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of sensory perception of pain	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
calcium ion transmembrane import into cytosol	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
excitatory chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
cellular response to L-glutamate	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
positive regulation of excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
long-term synaptic potentiation	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
protein insertion into membrane	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
regulation of calcium ion transport	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
calcium ion transmembrane transport	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
modulation of chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
monoamine transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to hypoxia	Sodium-dependent serotonin transporter	Homo sapiens (human)
neurotransmitter transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to nutrient	Sodium-dependent serotonin transporter	Homo sapiens (human)
memory	Sodium-dependent serotonin transporter	Homo sapiens (human)
circadian rhythm	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to xenobiotic stimulus	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to toxic substance	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of gene expression	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of serotonin secretion	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferation	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergic	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to estradiol	Sodium-dependent serotonin transporter	Homo sapiens (human)
social behavior	Sodium-dependent serotonin transporter	Homo sapiens (human)
vasoconstriction	Sodium-dependent serotonin transporter	Homo sapiens (human)
sperm ejaculation	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of neuron differentiation	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of cell cycle	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of organ growth	Sodium-dependent serotonin transporter	Homo sapiens (human)
behavioral response to cocaine	Sodium-dependent serotonin transporter	Homo sapiens (human)
enteric nervous system development	Sodium-dependent serotonin transporter	Homo sapiens (human)
brain morphogenesis	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin uptake	Sodium-dependent serotonin transporter	Homo sapiens (human)
membrane depolarization	Sodium-dependent serotonin transporter	Homo sapiens (human)
platelet aggregation	Sodium-dependent serotonin transporter	Homo sapiens (human)
cellular response to retinoic acid	Sodium-dependent serotonin transporter	Homo sapiens (human)
cellular response to cGMP	Sodium-dependent serotonin transporter	Homo sapiens (human)
regulation of thalamus size	Sodium-dependent serotonin transporter	Homo sapiens (human)
conditioned place preference	Sodium-dependent serotonin transporter	Homo sapiens (human)
sodium ion transmembrane transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
amino acid transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
fatty acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
icosanoid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
regulation of heart contraction	Cytochrome P450 2J2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2J2	Homo sapiens (human)
linoleic acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
organic acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of bitter taste	Taste receptor type 2 member 46	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Taste receptor type 2 member 46	Homo sapiens (human)
cellular response to amyloid-beta	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
monoatomic cation transport	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
brain development	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
visual learning	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
positive regulation of calcium ion transport into cytosol	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
propylene metabolic process	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calcium-mediated signaling	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
regulation of membrane potential	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
response to ethanol	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
regulation of synaptic plasticity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
regulation of neuronal synaptic plasticity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
protein heterotetramerization	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calcium ion homeostasis	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calcium ion transmembrane import into cytosol	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
excitatory chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
positive regulation of reactive oxygen species biosynthetic process	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
regulation of monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
response to glycine	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
positive regulation of excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
cellular response to amyloid-beta	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
startle response	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
response to amphetamine	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
brain development	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
learning or memory	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
memory	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
visual learning	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
response to xenobiotic stimulus	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
response to wounding	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
sensory perception of pain	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
calcium-mediated signaling	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
neurogenesis	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
protein catabolic process	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
sleep	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
directional locomotion	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
negative regulation of protein catabolic process	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
dopamine metabolic process	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
serotonin metabolic process	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
positive regulation of apoptotic process	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
response to ethanol	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
regulation of synaptic plasticity	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
regulation of neuronal synaptic plasticity	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
activation of cysteine-type endopeptidase activity	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
calcium ion transmembrane import into cytosol	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
excitatory chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
protein localization to postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
regulation of monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
positive regulation of excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
long-term synaptic potentiation	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
brain development	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
learning or memory	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
calcium-mediated signaling	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
response to ethanol	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
regulation of synaptic plasticity	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
regulation of neuronal synaptic plasticity	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
protein heterotetramerization	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
calcium ion transmembrane import into cytosol	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
excitatory chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
negative regulation of dendritic spine maintenance	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
regulation of monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
positive regulation of excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
long-term synaptic potentiation	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
brain development	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
response to wounding	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
calcium-mediated signaling	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
directional locomotion	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
negative regulation of protein catabolic process	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
regulation of synaptic plasticity	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
regulation of neuronal synaptic plasticity	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
neuromuscular process controlling balance	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
calcium ion transmembrane import into cytosol	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
excitatory chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
protein localization to postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
regulation of monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
positive regulation of excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
long-term synaptic potentiation	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
calcium ion transport	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
dendrite development	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
response to ethanol	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
rhythmic process	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
prepulse inhibition	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
negative regulation of dendritic spine development	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
calcium ion transmembrane transport	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
modulation of chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
lipid transport	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
nervous system development	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
G protein-coupled opioid receptor signaling pathway	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
regulation of neuron apoptotic process	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
protein homotrimerization	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
acetylcholine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine:sodium symporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine:sodium symporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
protein binding	Solute carrier family 22 member 1	Homo sapiens (human)
monoamine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
secondary active organic cation transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
organic cation transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
putrescine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
quaternary ammonium group transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
toxin transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
identical protein binding	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
(R)-carnitine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
glutamate-gated receptor activity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
glutamate binding	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
voltage-gated monoatomic cation channel activity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
calcium channel activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
monoatomic cation channel activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
glycine binding	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
neurotransmitter receptor activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
integrin binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monoatomic cation channel activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin:sodium:chloride symporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
protein binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monoamine transmembrane transporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
antiporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
syntaxin-1 binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
cocaine binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
sodium ion binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
identical protein binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
nitric-oxide synthase binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
actin filament binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
iron ion binding	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
isomerase activity	Cytochrome P450 2J2	Homo sapiens (human)
linoleic acid epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
heme binding	Cytochrome P450 2J2	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2J2	Homo sapiens (human)
G protein-coupled receptor activity	Taste receptor type 2 member 46	Homo sapiens (human)
bitter taste receptor activity	Taste receptor type 2 member 46	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calcium channel activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
amyloid-beta binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calcium ion binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calmodulin binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
glycine binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
glutamate binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
protein-containing complex binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
signaling receptor activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
ligand-gated monoatomic ion channel activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
amyloid-beta binding	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
zinc ion binding	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
amyloid-beta binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
zinc ion binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
glycine binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
glutamate binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
calcium channel activity	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
glycine binding	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
identical protein binding	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
protein phosphatase 2A binding	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
G protein-coupled opioid receptor activity	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
protein binding	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
basal plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
membrane	Solute carrier family 22 member 1	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
lateral plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
presynapse	Solute carrier family 22 member 1	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
presynaptic active zone membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
hippocampal mossy fiber to CA3 synapse	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
glutamatergic synapse	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
neuronal cell body	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
focal adhesion	Sodium-dependent serotonin transporter	Homo sapiens (human)
endosome membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
endomembrane system	Sodium-dependent serotonin transporter	Homo sapiens (human)
presynaptic membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
membrane raft	Sodium-dependent serotonin transporter	Homo sapiens (human)
synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
postsynaptic membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonergic synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
plasma membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
neuron projection	Sodium-dependent serotonin transporter	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Cytochrome P450 2J2	Homo sapiens (human)
extracellular exosome	Cytochrome P450 2J2	Homo sapiens (human)
cytoplasm	Cytochrome P450 2J2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2J2	Homo sapiens (human)
plasma membrane	Taste receptor type 2 member 46	Homo sapiens (human)
membrane	Taste receptor type 2 member 46	Homo sapiens (human)
ciliary membrane	Taste receptor type 2 member 46	Homo sapiens (human)
membrane	Taste receptor type 2 member 46	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)
cytoplasm	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synaptic vesicle	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
cell surface	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
postsynaptic density	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
dendrite	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
neuron projection	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synaptic cleft	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
terminal bouton	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
dendritic spine	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synapse	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
excitatory synapse	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synaptic membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synapse	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
neuron projection	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
synaptic vesicle	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
cell surface	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
postsynaptic density	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
cytoplasmic vesicle membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
presynaptic membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
dendritic spine	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
synaptic membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
glutamatergic synapse	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
cytoplasm	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
lysosome	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
late endosome	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
cytoskeleton	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
cell surface	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
postsynaptic density	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
neuron projection	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
synaptic membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
glutamatergic synapse	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
membrane	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
neuron projection	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
neuronal cell body	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
synapse	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
presynapse	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
glutamatergic synapse	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)
nuclear envelope	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
nuclear inner membrane	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
nuclear outer membrane	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
endoplasmic reticulum	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
endoplasmic reticulum membrane	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
lipid droplet	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
cytosol	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
postsynaptic density	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
membrane	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
growth cone	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
cytoplasmic vesicle	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
anchoring junction	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
postsynaptic density membrane	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
endoplasmic reticulum	Sigma non-opioid intracellular receptor 1	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID1210360	Drug metabolism in human liver microsomes assessed as dextrorphan formation measured as microsomal fraction unbound	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1220887	Inhibition of catalytic activity of recombinant human CYP2D6 expressed in Escherichia coli co-expressing P450 reductase assessed as hydroxybufuralol activity at 16 uM after <15 mins by HPLC analysis in presence of NADPH	2011	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6	Substituted imidazole of 5-fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine Inactivates cytochrome P450 2D6 by protein adduction.
AID1245598	Half life in human microsomes at 1 uM in presence of NADPH	2015	Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19	Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID54565	Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D3 expressed in Saccharomyces cerevisiae	2003	Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1	Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID1702155	n-Octanol/water distribution coefficient, logD of the compound at pH 7.4	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1773897	Half life in mouse liver microsomes preincubated for 5 mins followed by NADPH addition and measured after 5 to 60 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
AID1884504	Inhibition of CYP2D6 in human liver microsomes incubated for 15 to 40 mins in presence of NADPH	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1756359	Metabolic stability in human hepatocytes assessed as half life measured upto 120 mins by LC-MS/MS analysis	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID1611376	Half life in human liver microsomes at 1 uM in presence of NADPH generating system measured for 10 to 90 mins by LC-MS/MS analysis
AID1862576	Inhibition of CYP2D6 (unknown origin)
AID194779	Percent inhibition of veratridine-induced glutamate release in rat brain slices at 10000 nmol/L	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.
AID1247111	Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 3 to 50 mM Na+ to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 3 to 50 mM Na+	2015	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19	Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1313189	Half life in human liver microsomes at 3 uM in presence of NADPH by LC-MS/MS analysis	2016	Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15	Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
AID1635245	Half life in human liver microsomes at 3 uM preincubated with compound followed by NADPH addition by LC-MS/MS analysis	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1756362	Metabolic stability in rat hepatocytes assessed as half life measured upto 120 mins by LC-MS/MS analysis	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID1209250	Drug metabolism in human liver microsomes by multiple depletion curves method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1526773	Ratio of unbound maximal portal vein concentration in human at 60 mg, po to inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1526752	Passive membrane permeability by LC-MS/MS analysis based PAMPA	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID179824	Tested for the anticonvulsant activity administered 60 min orally before MES induction	1999	Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17	Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
AID1210362	Drug metabolism in human liver microsomes assessed as dextrorphan formation measured as intrinsic unbound clearance	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1209247	Drug metabolism in human liver microsomes assessed as intrinsic clearance per mg protein by multiple depletion curves method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID536851	Half life in human liver microsomes at 3 uM by LC-MS/MS analysis	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases.
AID1773898	Intrinsic clearance in mouse liver microsomes preincubated for 5 mins followed by NADPH addition and measured after 5 to 60 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
AID681153	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	2001	Chemical research in toxicology, Dec, Volume: 14, Issue:12	Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4.
AID203818	Binding affinity was measured as selectivity for sigma-1 site over muscarinic (M1) receptor in rat	1994	Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13	Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1174935	Behavioral effect in Wistar rat assessed as inhibition of nicotine-induced conditioned place preference at 10 mg/kg, ip administered during post-conditioning test phase on day 5 of nicotine treatment	2014	Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24	Synthesis, in vitro and in vivo studies, and molecular modeling of N-alkylated dextromethorphan derivatives as non-competitive inhibitors of α3β4 nicotinic acetylcholine receptor.
AID179553	Inhibitory effect against veratridine-induced glutamate release from rat brain slices	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.
AID1702152	Metabolic stability in human liver pooled microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1247112	Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 50 mM K+ to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 50 mM K+	2015	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19	Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1254927	Half life in human liver S9 microsomes in presence of NADPH by LC-MS/MS method	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	3-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID190134	Toxic dose causing 50% treated mice fall from the rotarod was evaluated; not calculated	1999	Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17	Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
AID1409611	AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay.	2020	Nature, 07, Volume: 583, Issue:7816	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1254933	Half life in human liver S9 microsomes in absence of NADPH by LC-MS/MS method	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	3-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID1526731	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.05 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1496417	Apparent half life in human liver microsomes at 3 uM	2018	Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11	BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
AID74203	Antitussive activity was evaluated by inhibition of irritant electrically-induced coughing by (po) administration in guinea pig	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	N-acyl-2-substituted-1,3-thiazolidines, a new class of non-narcotic antitussive agents: studies leading to the discovery of ethyl 2-[(2-methoxyphenoxy)methyl]-beta-oxothiazolidine-3-propanoate.
AID1526732	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.1 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1129361	Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis	2014	Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7	A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID588213	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID205276	Inhibition of [3H]saxitoxin binding to rat brain sodium channel	1999	Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17	Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
AID353103	Displacement of [3H]MK801 from NMDA receptor in rat brain neuronal membrane	2009	Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9	NMDA receptor affinities of 1,2-diphenylethylamine and 1-(1,2-diphenylethyl)piperidine enantiomers and of related compounds.
AID1247110	Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of H+ at pH 6.4 to 8.2 to IC50 for NMDA receptor in Wistar rat brain membranes in absence of H+ at pH 6.4 to 8.2	2015	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19	Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1702159	Clearance in mouse liver microsomes at pH 7.4 at 5 uM incubated upto 60 mins in presence of NADPH measured per mg of protein by LC-MS analysis	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1365724	Intrinsic clearance in human liver S9 microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis	2017	Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21	The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID1702153	Metabolic stability in mouse liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID205275	Inhibition of [3H]batrachotoxin binding to rat brain sodium channel	1999	Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17	Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
AID1409608	AUC (viral infection %) for SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).	2020	Nature, 07, Volume: 583, Issue:7816	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1365725	Intrinsic clearance in human liver S9 microsomes at 1 uM in absence of NADPH by LC-MS/MS analysis	2017	Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21	The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID1744242	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr in presence of 250 uM phenytoin liquid scintillation counting method	2021	Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1	Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID1652314	Inhibition of human CYP2D6 at 10 uM	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
AID54570	Inhibition of MAMC O-dealkylation mediated by human Cytochrome P450 2D6 expressed in human lymphoblastoid cell line	2003	Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1	Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID1759550	Metabolic stability in mouse liver microsomes assessed as half life	2021	Bioorganic & medicinal chemistry letters, 06-01, Volume: 41	Inhibitors of heat shock protein 70 (Hsp70) with enhanced metabolic stability reduce tau levels.
AID1210361	Drug metabolism in human liver microsomes assessed as dextrorphan formation measured as intrinsic clearance	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1773894	Half life in human liver microsomes preincubated for 5 mins followed by NADPH addition and measured after 5 to 60 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
AID1174942	Effect on basal locomotor activity in Wistar rat at 5 mg/kg, ip	2014	Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24	Synthesis, in vitro and in vivo studies, and molecular modeling of N-alkylated dextromethorphan derivatives as non-competitive inhibitors of α3β4 nicotinic acetylcholine receptor.
AID1247114	Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 1.3 mM Mg2+ to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 1.3 mM Mg2+	2015	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19	Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID699540	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1526759	Cmax in human at 60 mg, po	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID311933	Inhibition of ASM in rat PC12 cells assessed as residual activity at 10 uM	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1212341	Cytotoxicity against human Fa2N-4 cells by lactate dehydrogenase assay	2013	Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4	Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID317399	Displacement of [3H]pentazocine from sigma1 receptor in guinea pig membrane	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.
AID317400	Displacement of [3H]pentazocine from sigma1 receptor in guinea pig membrane in presence of phenytoin	2008	Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2	Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.
AID1702160	Clearance in rat liver microsomes at pH 7.4 at 5 uM incubated upto 60 mins in presence of NADPH measured per mg of protein by LC-MS analysis	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1174939	Behavioral effect in Wistar rat assessed as inhibition of expression of nicotine-induced locomotor sensitization at 5 to 10 mg/kg, ip administered on day 16 of pairing phase followed by nicotine treatment measured for 60 mins after compound treatment	2014	Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24	Synthesis, in vitro and in vivo studies, and molecular modeling of N-alkylated dextromethorphan derivatives as non-competitive inhibitors of α3β4 nicotinic acetylcholine receptor.
AID54564	Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D2 expressed in Saccharomyces cerevisiae	2003	Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1	Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID1426330	Half life in human liver microsomes at 1.5 uM in presence of NADPH by liquid chromatography/tandem mass spectrometric analysis	2017	Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3	Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.
AID1526771	Unbound maximal portal vein concentration of in human at 60 mg, po	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID311367	Permeability coefficient in human skin	2007	Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22	Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID1247113	Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 20 mM NH4+ to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 20 mM NH4+	2015	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19	Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1526760	Unbound Cmax in human at 60 mg, po	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1526751	Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1247109	Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 10 to 50 mM Tris to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 10 to 50 mM Tris	2015	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19	Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID404304	Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control	2008	Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11	Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1313195	Intrinsic clearance in human liver microsomes assessed per mg of protein at 3 uM in presence of NADPH by LC-MS/MS analysis	2016	Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15	Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
AID536762	Intrinsic clearance in human liver microsomes at 3 uM measured per mg of protein by LC-MS/MS analysis	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases.
AID1209248	Drug metabolism in human liver microsomes assessed as intrinsic clearance per mg protein by optimal design approach	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID54566	Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D4 expressed in Saccharomyces cerevisiae	2003	Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1	Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID1212315	Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence at 500 uM after 30 mins relative to control	2013	Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4	Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID1610344	Clearance in human liver microsomes at 1 uM in presence of NADPH generating system measured for 10 to 90 mins by LC-MS/MS analysis
AID1454611	Half life in mouse liver microsomes by LC-MS/MS method	2017	ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7	New Class of Antitrypanosomal Agents Based on Imidazopyridines.
AID1744243	Ratio of Ki for displacement of [3H]-(+)-pentazocine from sigma-1 receptor to Ki for displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes in presence of phenytoin	2021	Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1	Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID1365718	Half life in human liver S9 microsomes at 1 uM in absence of NADPH by LC-MS/MS analysis	2017	Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21	The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID1222793	Dissociation constant, pKa of the compound	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Which metabolites circulate?
AID1409613	Selectivity ratio: ratio of AUC (viral infection %) of SARS-CoV-2 in the Vero E6 cell line compared to AUC (cytotoxicity %) of compound against Vero E6 cells by MTT assay.	2020	Nature, 07, Volume: 583, Issue:7816	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1773895	Intrinsic clearance in human liver microsomes preincubated for 5 mins followed by NADPH addition and measured after 5 to 60 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
AID1756360	Metabolic stability in human hepatocytes assessed as clearance incubated up to 120 mins measured per million cells by LC-MS/MS analysis	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID1548950	Unbound hepatic clearance in rat liver microsomes	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10	Discovery of
AID1215672	Drug metabolism in pooled human hepatocytes assessed as aldehyde oxidase-mediated drug metabolism at 10 uM up to 120 mins by HPLC analysis in presence of 50 uM of hydralazine	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Hydralazine as a selective probe inactivator of aldehyde oxidase in human hepatocytes: estimation of the contribution of aldehyde oxidase to metabolic clearance.
AID1174934	Non-competitive inhibition of rat alpha3beta4 nAChR expressed in KX cells assessed as reduction in current by whole-cell patch clamp assay	2014	Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24	Synthesis, in vitro and in vivo studies, and molecular modeling of N-alkylated dextromethorphan derivatives as non-competitive inhibitors of α3β4 nicotinic acetylcholine receptor.
AID157456	Binding affinity was measured against phencyclidine (PCP) receptor in rat using [3H]TCP as radioligand	1994	Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13	Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1442001	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID1409614	Overall antiviral activity against SARS-CoV-2 (isolate France/IDF0372/2020) in the Vero E6 cell line at 48 h based on three assays 1) detection of viral RNA by qRT-PCR (targeting the N-gene), 2) plaque assay using lysate 3 days after addition of compound	2020	Nature, 07, Volume: 583, Issue:7816	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID311934	Dissociation constant, pKa of the compound	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1426327	Half life in mouse liver microsomes at 1.5 uM in presence of NADPH by liquid chromatography/tandem mass spectrometric analysis	2017	Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3	Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.
AID1496418	Intrinsic clearance in human liver microsomes at 3 uM	2018	Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11	BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
AID1409609	Cytotoxicity of compound against Vero E6 cells by MTT assay.	2020	Nature, 07, Volume: 583, Issue:7816	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1465450	Unbound intrinsic clearance in human liver microsomes at 10 uM preincubated for 5 mins followed by NADPH addition measured after 60 mins by HPLC-UV-MS analysis	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
AID699539	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1245597	Half life in human microsomes at 1 uM in absence of NADPH	2015	Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19	Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID1210359	Drug metabolism in human liver microsomes assessed as dextrorphan formation	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1526733	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake at 0.5 uM incubated for 2 mins by LC-MS/MS analysis relative to control empty vector transfected cells	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1682815	Metabolic stability in human liver microsomes assessed as half life
AID1409607	IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).	2020	Nature, 07, Volume: 583, Issue:7816	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
AID1210069	Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1610343	Half life in human liver microsomes at 1 uM in presence of NADPH generating system measured for 10 to 90 mins by LC-MS/MS analysis
AID1247108	Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 30 uM spermine to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 30 uM spermine	2015	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19	Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1209258	Drug metabolism in human liver microsomes assessed as maximum rate of reaction per mg protein by multiple depletion curves method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID212532	Lethal dose in rats	1999	Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17	Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
AID262947	Inhibition of human CYP2D6 expressed in Escherichia coli JM109	2006	Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8	Catalytic site prediction and virtual screening of cytochrome P450 2D6 substrates by consideration of water and rescoring in automated docking.
AID1756363	Metabolic stability in rat hepatocytes assessed as intrinsic clearance incubated up to 120 mins measured per million cells by LC-MS/MS analysis	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
AID226359	Displacement of [3H]BTX from sodium channel of rat cerebral cortex synaptosomes	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.
AID699541	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID204634	Inhibition of [3H](+)-pentazocine binding to Sigma receptor type 1	2004	Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7	Synthesis of potent sigma-1 receptor ligands via fragmentation of dextromethorphan.
AID1247107	Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis	2015	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19	Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1526772	Ratio of unbound Cmax in human at 60 mg, po to inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis	2019	Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21	Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1209259	Drug metabolism in human liver microsomes assessed as maximum rate of reaction per mg protein by optimal design approach	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID142870	Binding affinity was measured against muscarinic (M2) receptor at 10 uM in rat using [3H]QN as radioligand	1994	Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13	Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1209251	Drug metabolism in human liver microsomes by optimal design approach	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID54562	Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D1 expressed in Saccharomyces cerevisiae	2003	Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1	Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID1611377	Clearance in human liver microsomes at 1 uM in presence of NADPH generating system measured for 10 to 90 mins by LC-MS/MS analysis
AID1365717	Half life in human liver S9 microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis	2017	Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21	The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID313147	Reduction in pain intensity in diabetic neuropathy patient	2007	Journal of medicinal chemistry, May-31, Volume: 50, Issue:11	N-methyl-D-aspartate antagonists and neuropathic pain: the search for relief.
AID588211	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1702154	Metabolic stability in rat liver microsomes assessed as half-life at 5 uM incubated upto 60 mins in presence of beta-NADPH by LC-MS analysis	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1210363	Drug metabolism in human liver microsomes assessed as dextrorphan formation measured as plasma fraction unbound	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1212314	Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence after 30 mins	2013	Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4	Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID353104	Ratio of Ki for rat brain NMDA receptor in presence of 100 uM spermine to Ki for rat brain NMDA receptor in absence of spermine	2009	Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9	NMDA receptor affinities of 1,2-diphenylethylamine and 1-(1,2-diphenylethyl)piperidine enantiomers and of related compounds.
AID74201	Antitussive activity was evaluated by inhibition of irritant aerosol-induced coughing by (po) administration in guinea pig	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	N-acyl-2-substituted-1,3-thiazolidines, a new class of non-narcotic antitussive agents: studies leading to the discovery of ethyl 2-[(2-methoxyphenoxy)methyl]-beta-oxothiazolidine-3-propanoate.
AID588212	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1210358	Drug metabolism in human liver microsomes assessed as dextrorphan formation measured per mg of microsomal protein	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.
AID1702156	Inhibition of human ERG by fluorescence polarization assay	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID19006	Calculated membrane partition coefficient (Kmemb)	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID1209236	Drug metabolism in assessed as human CYP2D6-mediated maximum rate of reaction per mg protein	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1209262	Drug metabolism in assessed as human CYP2D6-mediated intrinsic clearance per mg protein	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1702158	Clearance in human liver pooled microsomes at pH 7.4 at 5 uM incubated upto 60 mins in presence of NADPH measured per mg of protein by LC-MS analysis	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1174937	Toxicity in Wistar rat assessed as inhibition of conditioned place preference at 10 mg/kg, ip in absence of nicotine preconditioning	2014	Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24	Synthesis, in vitro and in vivo studies, and molecular modeling of N-alkylated dextromethorphan derivatives as non-competitive inhibitors of α3β4 nicotinic acetylcholine receptor.
AID1209237	Drug metabolism in assessed as human CYP2D6-mediated metabolism	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1442006	Ratio of Kii for human OCT1-ASP+-inhibitor complex to Kis for human OCT1-inhibitor complex by Lineweaver-Burk plot analysis	2017	Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7	Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID156805	The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex.	1998	Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3	Quantitative analysis of the structural requirements for blockade of the N-methyl-D-aspartate receptor at the phencyclidine binding site.
AID1744232	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method	2021	Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1	Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
AID145105	Binding affinity was measured against N-methyl-D-aspartate (NMDA) receptor in rat using [3H]CGS-19,755 as radioligand at 10 uM	1994	Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13	Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
AID1773899	Hepatic clearance in mouse liver microsomes preincubated for 5 mins followed by NADPH addition and measured after 5 to 60 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
AID1773896	Hepatic clearance in human liver microsomes preincubated for 5 mins followed by NADPH addition and measured after 5 to 60 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
AID1635243	Intrinsic clearance in human liver microsomes assessed per mg protein at 3 uM preincubated with compound followed by NADPH addition measured after 5 to 45 mins by LC-MS/MS analysis	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1682813	Metabolic stability in human liver microsomes assessed as intrinsic clearance
AID226516	Protective index (PI) is the ratio of TD50 in the rotarod test over the ED50 in the anticonvulsant test;not calculated	1999	Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17	Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
AID1702161	Drug metabolism assessed as human recombinant CYP3A4-mediated clearance at pH 7.4 at 5 uM incubated upto 60 mins in presence of NADPH by LC-MS analysis	2018	Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4	Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346601	Human GluN2C (Ionotropic glutamate receptors)	2007	The Journal of physiology, May-15, Volume: 581, Issue:Pt 1	Subunit-specific mechanisms and proton sensitivity of NMDA receptor channel block.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	209 (10.95)	18.7374
1990's	468 (24.53)	18.2507
2000's	594 (31.13)	29.6817
2010's	498 (26.10)	24.3611
2020's	139 (7.29)	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	342 (16.93%)	5.53%
Reviews	122 (6.04%)	6.00%
Case Studies	179 (8.86%)	4.05%
Observational	3 (0.15%)	0.25%
Other	1,374 (68.02%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (136)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Randomized Drug Interaction Study of RO4929097 for Advanced Solid Tumors [NCT01218620]	Phase 1	17 participants (Actual)	Interventional	2010-09-30	Completed
Endobiotics for Phenotyping of Human Cytochrome P450 Enzymes: Use of Metabolomics for the Identification of New CYP2D6 Endogenous Biomarkers in Healthy Volunteers [NCT04188028]		40 participants (Actual)	Interventional	2019-01-01	Completed
Licorice Botanical Dietary Supplements - Metabolism and Safety in Women [NCT03948243]	Phase 1	19 participants (Actual)	Interventional	2019-04-01	Completed
The Potential Therapeutic Effects of add-on Low Dose Dextromethorphan and Memantine in Patients With Amphetamine-type Stimulants Use Disorder [NCT03729128]	Phase 1/Phase 2	85 participants (Actual)	Interventional	2018-07-24	Completed
Evaluation of the Effect of LY3871801 on the Pharmacokinetics of CYP450 Substrates and an OAT1/3 Substrate in Healthy Participants [NCT05602675]	Phase 1	39 participants (Actual)	Interventional	2022-11-02	Completed
A Phase 1, Open-label, Drug Interaction Study to Evaluate the Effect of Guselkumab (CNTO 1959) on Cytochrome P450 Enzyme Activities Following a Single Subcutaneous Administration in Subjects With Moderate to Severe Plaque-type Psoriasis [NCT02397382]	Phase 1	16 participants (Actual)	Interventional	2015-06-18	Completed
Effects of Multiple Doses of Abemaciclib on the Pharmacokinetics of Cytochrome P450 (CYP) 1A2, CYP2C9, CYP2D6, and CYP3A Substrates (Caffeine, Warfarin, Dextromethorphan, and Midazolam) in Cancer Patients [NCT02688088]	Phase 1	48 participants (Actual)	Interventional	2016-03-08	Completed
Psilocybin-facilitated Treatment for Chronic Pain [NCT05068791]	Early Phase 1	30 participants (Anticipated)	Interventional	2023-11-01	Recruiting
[NCT02391688]	Phase 1	30 participants (Actual)	Interventional	2014-11-30	Completed
Impact of Nuedexta on Bulbar Physiology and Function in ALS [NCT03883581]	Phase 1/Phase 2	28 participants (Actual)	Interventional	2019-07-25	Completed
An Open-Label Drug Interaction Study in Healthy Subjects to Evaluate the Effects of Multiple Doses of JNJ55308942 on the Cytochrome P450 CYP3A4, CYP2D6 and CYP2C19 Activity and on the Pharmacokinetics of Levonorgestrel/Ethinyl Estradiol [NCT03547024]	Phase 1	14 participants (Actual)	Interventional	2018-06-08	Completed
Fluoxetine/Dextromethorphan in Obsessive-Compulsive and Related Disorders: an Open-Label Crossover Pilot Study [NCT04899687]	Phase 2	60 participants (Anticipated)	Interventional	2022-01-20	Recruiting
An Open-Label Study to Assess the Long-term Safety and Efficacy of AXS-05 in Subjects With Major Depressive Disorder [NCT04039022]	Phase 3	876 participants (Actual)	Interventional	2019-07-08	Completed
A Double-blind, Placebo-Controlled, Randomized Study of the Efficacy of Dextromethorphan as Add-On Therapy to Risperidone Versus Risperidone Alone in Patients With Schizophrenia [NCT01189006]	Phase 2/Phase 3	161 participants (Actual)	Interventional	2005-01-31	Completed
The Reno-protective and Cardiovascular Effect of Dextromethorphan and Silymarin in Patients With Chronic Kidney Disease [NCT01091324]	Phase 3	45 participants (Anticipated)	Interventional	2010-01-31	Active, not recruiting
Dextromethorphan in Fibromyalgia [NCT03538054]	Phase 2	27 participants (Actual)	Interventional	2018-06-26	Completed
Effect of Acute Ethanol Consumption on The Activity of Major Cytochrome P450 Enzymes, NAT2 and P-glycoprotein [NCT02515526]		16 participants (Actual)	Interventional	2015-06-30	Completed
A Study to Evaluate the Effect of Multiple Doses of 500 mg of BIRT 2584 XX Tablets on the Pharmacokinetic Parameters of Warfarin, Omeprazole, Caffeine, and Dextromethorphan Dosed Orally and Midazolam Dosed IV, in Healthy Male Volunteers [NCT02256813]	Phase 1	20 participants (Actual)	Interventional	2005-09-30	Completed
Cocktail Phenotypic Approach to Explore Antidepressant Pharmacokinetic Variability: a Pilot Study [NCT02438072]		100 participants (Anticipated)	Interventional	2014-12-31	Recruiting
Evaluation of the Effect of Ixekizumab on the Pharmacokinetics of Cytochrome P450 Substrates in Patients With Moderate-to-Severe Plaque Psoriasis [NCT02993471]	Phase 1	28 participants (Actual)	Interventional	2016-12-22	Completed
Single Centre Open-label, Non-randomised, 3-treatment, 2-period, Pharmacokinetic Drug Interaction Study of Single Oral Dose of Acoziborole With Sequential Co-administration of Midazolam and Dextromethorphan in Healthy Male Participants [NCT05947604]	Phase 1	20 participants (Actual)	Interventional	2023-02-09	Completed
Trial of Naltrexone and Dextromethorphan for Gulf War Veterans Illnesses [NCT02206490]	Phase 2	60 participants (Actual)	Interventional	2012-01-31	Completed
A PLACEBO-CONTROLLED, DOUBLE-BLIND, RANDOMIZED, PARALLEL GROUP PILOT STUDY TO EVALUATE THE EFFICACY OF DEXTROMETHORPHAN HYDROBROMIDE ON ACUTE COUGH IN A PEDIATRIC POPULATION [NCT02651116]	Phase 4	131 participants (Actual)	Interventional	2016-02-25	Terminated(stopped due to The study was prematurely discontinued due to slow enrollment during the 2019/2020 cold season. No safety or efficacy concerns led to the decision to terminate)
Effects of Type 2 Diabetes on CYP450s Activities; Intersubject Variability in Drug Metabolism. [NCT02291666]	Phase 4	73 participants (Actual)	Interventional	2015-04-30	Completed
A Phase I Multiple Dose Trial to Investigate Safety With Special Emphasis on ECG Effects and Tolerability After Oral Doses of 30 mg q.i.d. and 90 mg q.i.d. Dextromethorphan Hydrobromide Monohydrate (2 mg/mL Syrup) in Healthy Male and Female Subjects for 2 [NCT02191176]	Phase 1	48 participants (Actual)	Interventional	2009-06-30	Completed
Risk of Phenoconversion in Genetic Extensive Metabolizers Healthy Volunteers Carriers of One Fully-Functional and One Non-Functional Allele Versus Carriers of Two Fully-Functional Alleles [NCT03054220]		34 participants (Actual)	Interventional	2016-07-31	Completed
Clinical Trials on Evaluate the Red Ginseng and Fermented-Red Ginseng Affect to Drug Metabolizing Enzyme and Transporter in Healthy Volunteers; Open-label, Parallel Group [NCT02056743]	Phase 1	30 participants (Actual)	Interventional	2013-09-30	Completed
A Phase 2a, Double-blind, Randomized, Placebo-controlled, Crossover Study to Evaluate the Safety and Efficacy of AVP-923 (Dextromethorphan/Quinidine) in the Treatment of Levodopa-induced Dyskinesia in Parkinson's Disease Patients. [NCT01767129]	Phase 2	14 participants (Actual)	Interventional	2013-10-16	Completed
Evaluation of the Effects of Single Oral Dose and Multiple Oral Doses of BI 201335 NA on Cytochrome P450 and P-glycoprotein Activity Using a Probe Drug Cocktail. An Open-label, Single-arm Phase I Study in Healthy Human Volunteers [NCT02182336]	Phase 1	23 participants (Actual)	Interventional	2008-06-30	Completed
An Open-label, 2-cycle Clinical Study to Evaluate the Drug Interaction Between Itraconazole or Dextromethorphan and IBI351 in Healthy Subjects [NCT05699993]	Phase 1	24 participants (Actual)	Interventional	2023-03-10	Completed
Dextromethorphan as a Novel Non-opioid Adjunctive Agent for Pain Control in Medication Abortion: a Randomized Controlled Trial [NCT03480009]	Phase 3	156 participants (Actual)	Interventional	2018-07-28	Completed
Dextromethorphan Enhances the Therapeutic Efficacy of Valoproate in Bipolar Disorder Patients [NCT01188265]	Phase 3	300 participants (Actual)	Interventional	2007-06-30	Completed
A Phase 1, Randomized, Single-Dose, 3-Way, Crossover Study to Compare the Relative Bioavailability, Pharmacokinetics, Safety and Tolerability of AVP-923 (Dextromethorphan Hydrobromide and Quinidine Sulfate Capsules) Administered in Applesauce or Via a Nas [NCT03381664]	Phase 1	17 participants (Actual)	Interventional	2017-11-28	Completed
Combined Therapy of Methadone and Dextromethrophan: A Novel Strategy for the Treatment of Opioid Dependence [NCT01189097]	Phase 3	1,500 participants (Anticipated)	Interventional	2008-04-30	Recruiting
Phase 1, Open-label, One-arm, Fixed-sequence Study to Evaluate the Effects of 90 mg Intravenous Infusions of GC4419 on the Single Dose Pharmacokinetics of Dextromethorphan in Healthy Adult Subjects [NCT03792971]	Phase 1	13 participants (Actual)	Interventional	2019-02-10	Completed
A Phase 1, Randomized, Open-Label, Two-Way Crossover Study To Evaluate The Steady-State Effect Of Dimebon [PF-01913539] On The Single-Dose Pharmacokinetics Of The CYP2D6 Substrate Dextromethorphan In Healthy Subjects [NCT00788047]	Phase 1	14 participants (Actual)	Interventional	2008-11-30	Completed
A Phase I, Single Dose, Controlled Two-way Crossover Study to Evaluate the Relative Bioavailability of Orally Administered Dextromethorphan Syrup (21 mg Dextromethorphan Hydrobromide Monohydrate) in Comparison to Dextromethorphan Soft Pastilles (21 mg Dex [NCT02191709]	Phase 1	18 participants (Actual)	Interventional	2009-01-31	Completed
A Fixed-Sequence Trial to Examine the Effect of Multiple-Dose CT1812 Administration on Standard Probes of CYP2C19 (Omeprazole), CYP2C9 (Tolbutamide), CYP2D6 (Dextromethorphan), and CYP3A4/5 (Midazolam) Activity in Healthy Adult Volunteers [NCT03716427]	Phase 1	16 participants (Actual)	Interventional	2016-11-10	Completed
Combination of Dextromethorphan and Memantine in Treating Bipolar Disorder [NCT03039842]	Phase 3	300 participants (Anticipated)	Interventional	2013-01-01	Enrolling by invitation
A Placebo-controlled, Single-blind, Randomised Study to Investigate the Safety, Tolerability, Pharmacokinetics and Drug Interaction of GSK1034702 After Repeat Doses in Healthy Subjects [NCT00950586]	Phase 1	48 participants (Actual)	Interventional	2009-08-24	Completed
A Randomized Clinical Trial to Assess the Effects of Single Doses of MK2637 and Dextromethorphan on Cerebral Cortex Excitability in Healthy Subjects [NCT00934466]	Phase 1	15 participants (Actual)	Interventional	2009-07-31	Completed
An Open-label Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Cytochrome P450 Probe Drugs in Healthy Adult Subjects [NCT00964106]	Phase 1	87 participants (Actual)	Interventional	2009-08-26	Completed
An Abiraterone Acetate Plus Prednisone Drug-Drug Interaction Study With Dextromethorphan and Theophylline in Patients With Metastatic Castration-Resistant Prostate Cancer [NCT01017939]	Phase 1	34 participants (Actual)	Interventional	2010-01-31	Completed
A Phase 1 Open-label Study to Evaluate the Effect of Multiple Doses of Enzalutamide on the Pharmacokinetics of Substrates for CYP1A2 and CYP2D6 in Male Subjects With Prostate Cancer [NCT02225093]	Phase 1	12 participants (Actual)	Interventional	2013-10-02	Completed
A Two-cohort, Two-part, Phase 1, Multicenter, Open-label, Fixed-sequence, Drug-Drug Interaction and QTc Assessments of Sitravatinib Followed by Combination Treatment With Nivolumab in Patients With Advanced Solid Malignancies [NCT04887194]	Phase 1	40 participants (Actual)	Interventional	2021-03-26	Completed
A Double-Blind, Randomized, Placebo-Controlled, Multicenter Study to Assess the Safety and Efficacy and to Determine the Pharmacokinetics of Two Doses of AVP-923 (Dextromethorphan/Quinidine) in the Treatment of Pseudobulbar Affect (PBA) in Patients With A [NCT00573443]	Phase 3	326 participants (Actual)	Interventional	2007-12-31	Completed
Randomized Clinical Trial to Evaluate Guidelines for Acute Rhinosinusitis (Phase IV Study) [NCT00377403]	Phase 4	172 participants (Actual)	Interventional	2006-10-31	Completed
A Phase 1, Open-label, Drug Interaction Study to Evaluate the Effect of Ustekinumab on Cytochrome P450 Enzyme Activities Following Induction and Maintenance Dosing in Participants With Active Crohn's Disease or Ulcerative Colitis. [NCT03358706]	Phase 1	57 participants (Anticipated)	Interventional	2018-02-02	Suspended(stopped due to unavailability of probe substrates)
Trial of Dextromethorphan in Rett Syndrome [NCT00593957]	Phase 2	38 participants (Actual)	Interventional	2004-08-31	Terminated(stopped due to Study changed to a placebo controlled trial of dextromethorphan)
A Phase I Study to Evaluate the Effect of Darunavir/Ritonavir and Lopinavir/Ritonavir on GSK2248761 Pharmacokinetics and to Assess the Effect of GSK2248761 on CYP450 Probe Drugs in Healthy Adult Subjects [NCT00920088]	Phase 1	24 participants (Actual)	Interventional	2009-06-30	Completed
A Phase 1 Dose-Escalation Study of the Safety and Pharmacokinetics of GDC-0973/XL518 Administered Orally Daily to Subjects With Solid Tumors [NCT00467779]	Phase 1	119 participants (Actual)	Interventional	2007-05-31	Completed
Effect of Concomitant Administration of BMS-708163 on the Pharmacokinetics of Midazolam, Warfarin, Caffeine, Omeprazole and Dextromethorphan in Healthy Male Subjects by Administration of a Modified Cooperstown Cocktail [NCT00726726]	Phase 1	22 participants (Actual)	Interventional	2008-08-31	Completed
A Phase II, Fixed-sequenced, Open- Label, Research Study to Assess Pharmacokinetic Drug Interactions of AEGR-733 on Lipid-lowering Therapies in Healthy Volunteers [NCT00359281]	Phase 2	125 participants (Actual)	Interventional	2006-03-31	Completed
An Open-Label, 2-Part, Multicenter, Post-marketing Study to Evaluate the Effect of Moderately or Severely Active Ulcerative Colitis or Crohn's Disease on Cytochrome P-450 Enzyme Substrates Compared to Healthy Subjects and the Effect of Vedolizumab Treatme [NCT02760615]	Phase 4	0 participants (Actual)	Interventional	2016-11-01	Withdrawn(stopped due to No enrollment)
Evaluating the Efficacy of Dextromethorphan/Quinidine in Treating Irritability in Huntington's Disease [NCT03854019]	Phase 3	20 participants (Actual)	Interventional	2019-08-05	Completed
A Phase IIa, Dose-finding, Double-blind, Placebo-controlled, Double-dummy, Randomized, Eightfold Cross-over Study to Investigate the Glucose Lowering Effects of Dextromethorphan Alone or in Combination With Sitagliptin in Subjects With Type 2 Diabetes Mel [NCT01936025]	Phase 2	34 participants (Actual)	Interventional	2013-10-31	Completed
NMDA Receptor Antagonist Treatment of Neurodegenerative Disease [NCT00001365]	Phase 2	42 participants	Interventional	1993-07-31	Completed
Clinical Trials in Orofacial Neuralgias [NCT00001725]	Phase 2	100 participants	Interventional	1997-12-31	Completed
Assessing the Pharmacokinetics and Drug Interaction Liability of Kratom, an Opioid-like Natural Product [NCT04392011]	Early Phase 1	15 participants (Actual)	Interventional	2019-10-09	Completed
Dextromethorphan as an Augmentation Agent in Treatment-resistant Schizophrenia: A Randomized, Group Sequential Adaptive Design, Controlled Clinical Trial [NCT05944510]	Phase 4	72 participants (Anticipated)	Interventional	2023-08-31	Recruiting
Antagonists NMDA in Relay to Ketamine in Neuropathic Pain [NCT01602185]	Phase 2	7 participants (Actual)	Interventional	2012-05-31	Completed
A Phase 2, Double-blind, Randomized, Placebo-controlled, Four-arm, Multicenter, Dose-finding Study to Assess the Safety and Efficacy of Three Dose Levels of AVP-923 (Dextromethorphan/Quinidine) in the Treatment of Central Neuropathic Pain in Patients With [NCT01324232]	Phase 2	209 participants (Actual)	Interventional	2011-09-08	Completed
The Study of Risk Factors and Intervention for Children With Chronic Irritability - a Preliminary Approach With Epidemiological, Neuropsychological and Neuroinflammation Studies [NCT05043805]	Phase 4	120 participants (Anticipated)	Interventional	2021-05-09	Enrolling by invitation
A Prospective Randomized Double-blind Placebo Controlled Trial; Does Pre and Postoperative Dextromethorphan Reduce Post-tonsillectomy Pain in Children? [NCT02727491]	Phase 4	85 participants (Actual)	Interventional	2012-03-31	Completed
¹³C - Dextromethorphan (DM) Breath Test for Determination of CYP2D6 Enzyme Activity in Patients Receiving Tamoxifen [NCT00873366]		92 participants (Actual)	Observational	2009-05-31	Terminated(stopped due to Funding issues)
An Open Label Phase 1, Randomized Cross Over Trial To Estimate The Effect Of PF- 00299804 On The Pharmacokinetics Of Dextromethorphan In Healthy Volunteers [NCT00999817]	Phase 1	14 participants (Actual)	Interventional	2009-11-30	Completed
A Randomized, Double-Blind 4-Week Study to Evaluate the Impact of AXS-05 on Smoking Behavior [NCT03471767]	Phase 2	58 participants (Actual)	Interventional	2018-03-25	Completed
Repurposing of Dextromethorphan as an Adjunct Therapy in Patients With Major Depressive Disorder: A Randomized, Group Sequential, Adaptive Design, Controlled Clinical Trial [NCT05181527]	Phase 4	60 participants (Actual)	Interventional	2022-02-10	Completed
A Randomized, Parallel-Group, Double-Blind, Placebo-Controlled, Single-Dose, Pilot Study To Evaluate Efficacy Of Dextromethorphan Hydrobromide On Acute Cough In A Pediatric Population [NCT01257542]	Phase 4	140 participants (Actual)	Interventional	2010-12-31	Terminated(stopped due to See termination reason in detailed description.)
A Double-Blind Placebo-Controlled Trial of Dextromethorphan for Treatment of Major Depressive Disorder [NCT02860962]	Phase 1	4 participants (Actual)	Interventional	2016-08-31	Completed
[NCT00333242]	Phase 1	40 participants (Actual)	Interventional	2002-09-30	Active, not recruiting
A Pilot Study of Dextromethorphan for the Prevention and Treatment of Methotrexate Neurotoxicity [NCT00176553]		20 participants (Anticipated)	Interventional	2003-03-31	Terminated(stopped due to slow accrual)
An Open-Label Study to Assess the Long-term Safety and Efficacy of AXS-05 in Subjects With Treatment Resistant Depression [NCT04634669]	Phase 2	186 participants (Actual)	Interventional	2020-09-23	Completed
An Open-Label Study to Assess the Long-term Safety and Efficacy of AXS-05 in Subjects With Dementia of the Alzheimer's Type [NCT04947553]	Phase 3	260 participants (Anticipated)	Interventional	2021-06-17	Enrolling by invitation
A Phase 2, Multicenter, Randomized, Double-blind, Placebo-controlled Study to Assess the Efficacy, Safety, and Tolerability of AVP-786 (Deuterium Modified Dextromethorphan Hydrobromide/Quinidine Sulfate) as an Adjunctive Therapy in Patients With Major Dep [NCT02153502]	Phase 2	206 participants (Actual)	Interventional	2014-07-31	Completed
Recombinant Human Growth Hormone Therapy and Drug Metabolism [NCT00458991]		9 participants (Actual)	Observational	2001-06-30	Completed
Non-Invasive Assessment of Opioid Analgesia in Children With Sickle Cell Disease [NCT00513864]	Phase 4	0 participants (Actual)	Interventional	2006-11-30	Withdrawn(stopped due to lack of funding)
Treatment Efficacy in Dextromethorphan, Memantine Monotherapy, or Combined Use of Dextromethorphan and Memantine in Patients With Amphetamine-type Stimulants Use Disorder [NCT04687566]	Phase 2/Phase 3	120 participants (Anticipated)	Interventional	2020-08-11	Recruiting
Evaluating the Effects of Tipranavir (With Ritonavir) Capsule and Liquid Formulation on Cytochrome P450 and P-glycoprotein Activity Using a Biomarker Cocktail in Healthy Human Volunteers [NCT02243553]	Phase 1	34 participants (Actual)	Interventional	2006-01-31	Completed
Effectiveness of Antitussives, Anticholinergics and Honey Versus Usual Care in Adults With Uncomplicated Acute Bronchitis. [NCT03738917]	Phase 4	668 participants (Actual)	Interventional	2019-02-01	Completed
The Effect of Imlunestrant on CYP2C8, CYP2C19, CYP2D6, P-gp, and BCRP Activity and the Effect of P-gp Inhibition on Imlunestrant Pharmacokinetics in Healthy Women of Non-childbearing Potential [NCT05444556]	Phase 1	113 participants (Actual)	Interventional	2022-07-07	Completed
Effect of Honey and Dextromethorphan on Nocturnal Cough and Sleep Quality for Coughing Children and Their Parents [NCT00127686]	Phase 1	105 participants (Actual)	Interventional	2005-09-30	Completed
Characterization of Pain Processing Mechanisms in Irritable Bowel Syndrome [NCT00108446]	Phase 2	0 participants	Interventional	2003-10-31	Completed
An Open-Label, Multiple-Dose, Non-Randomized Study to Assess the Drug-Drug Interactions of Proellex® (CDB-4124) With Cytochrome P450 Isoenzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 in Healthy Female Subjects [NCT00741468]	Phase 1	18 participants (Actual)	Interventional	2008-07-31	Completed
Dextromethorphan Versus Placebo for Neuropathic Pain [NCT00001344]	Phase 2	129 participants	Interventional	1993-03-31	Completed
A Pilot Trial to Evaluate the Effects of Dextromethorphan in Patients Suffering From Cancer-Related Fatigue [NCT00176540]		30 participants (Anticipated)	Interventional	2003-10-31	Terminated(stopped due to slow accrual)
Anti-Inflammation & Vascular Endothelial Protection Effects of Dextromethorphan on Heavy Smoker [NCT00605605]	Phase 4	40 participants (Actual)	Interventional	2005-03-31	Completed
Effect of N-methyl D-aspartate (NMDA) Receptor Antagonist Dextromethorphan on Opiods Analgesia and Tolerance in Pediatric Intensive Care Unit Patients [NCT01553435]		36 participants (Anticipated)	Interventional	2011-01-31	Active, not recruiting
The Effects of an NMDA-Receptor Antagonist in Idiopathic Voice Disorders [NCT00055549]	Phase 1	65 participants	Interventional	2003-03-04	Completed
Pathogenesis of Rett Syndrome: Natural History and Treatment [NCT00069550]	Phase 3	90 participants	Interventional	2004-09-30	Recruiting
Dextromethorphan in Chemotherapy-induced Peripheral Neuropathy Management [NCT02271893]	Phase 2	19 participants (Actual)	Interventional	2014-11-25	Terminated(stopped due to Recruitment difficulties)
The Experimental Treatment of Bulbar Dysfunction in Amyotrophic Lateral Sclerosis (ALS) [NCT01806857]	Phase 2	90 participants (Actual)	Interventional	2013-04-30	Completed
Placebo Controlled Trial of Dextromethorphan in Rett Syndrome [NCT01520363]	Phase 2	57 participants (Actual)	Interventional	2012-03-31	Completed
Antitussive Effect of a Naturally Flavored, Multi-Component Syrup Containing Diphenhydramine, Compared With Dextromethorphan and Placebo [NCT02062710]	Phase 4	22 participants (Actual)	Interventional	2014-01-31	Completed
A Phase 1, Open-label, 2-period Fixed-sequence Study to Evaluate the Effect of Multiple Doses of SHP620 (Maribavir) on the Pharmacokinetics of Digoxin and Dextromethorphan in Healthy Adult Subjects [NCT02775240]	Phase 1	18 participants (Actual)	Interventional	2016-07-21	Completed
A Study to Assess the Safety, Tolerability and Effectiveness of Nuedexta (Dextromethorphan 20 mg/Quinidine 10 mg) in the Treatment of Pseudobulbar Affect (PBA) [NCT01799941]	Phase 4	367 participants (Actual)	Interventional	2013-02-28	Completed
Effect of Chronic Intermittent Nocturnal Hypoxia on Hepatic Drug Biotransformation in Children With Obstructive Sleep Apnea [NCT00310323]		69 participants (Actual)	Interventional	2003-01-31	Completed
A Randomized, Placebo-Controlled Study to Evaluate the Efficacy of Perioperative Dextromethorphan Compared to Placebo for the Treatment of Postoperative Pain [NCT05278494]		160 participants (Anticipated)	Interventional	2022-09-15	Recruiting
A Phase 1, Open-Label, Sequential Study of the Effect of Multiple Doses of Isavuconazole on the Pharmacokinetics of a Single Dose of Dextromethorphan in Healthy Adult Subjects [NCT01651325]	Phase 1	24 participants (Actual)	Interventional	2012-05-31	Completed
[NCT01731067]	Phase 1	10 participants (Anticipated)	Interventional	2012-11-30	Completed
Dextromethorphan Added on Methylphenidate in the Treatment of the Patients With ADHD [NCT01787136]		0 participants	Expanded Access		No longer available
Clinical Protocol of a Prospective, Open-label Study to Assess the Safety and Efficacy of Nuedexta (Dextromethorphan/Quinidine) in the Treatment of Pseudobulbar Affect (PBA) in Patients With Alzheimer's Disease [NCT01832350]	Phase 4	34 participants (Actual)	Interventional	2012-08-28	Terminated(stopped due to Sponsor decided to stop study early)
A Phase IIa, Double-blind, Placebo-controlled, Randomised, Fourfold Crossover Study to Investigate the Glucose Lowering Effects of Dextromethorphan and Amantadine in Subjects With Type 2 Diabetes Mellitus (T2DM) After an Oral Glucose Tolerance Test [NCT01441986]	Phase 2	20 participants (Actual)	Interventional	2011-09-30	Completed
A Phase 2, Multicenter, Randomized, Double-blind, Placebo-controlled Study to Assess the Safety, Tolerability, and Efficacy of AVP-786 for the Treatment of Disinhibition in Patients With Neurodegenerative Disorders [NCT02534038]	Phase 2	1 participants (Actual)	Interventional	2015-12-31	Terminated(stopped due to The study was terminated prematurely because of difficulty with recruiting.)
Effects of Dextromethorphan on Opioid Tolerance in Methadone Patients [NCT00000352]	Phase 2	0 participants	Interventional	1996-12-31	Completed
Nuedexta for Neurobehavioral Symptoms of Adults With Autism Spectrum Disorder [NCT01630811]	Phase 2	13 participants (Actual)	Interventional	2012-01-24	Completed
The Effects of Multiple Dose Fluoxetine and Metabolites on CYP1A2, CYP2C19, CYP2D6 and CYP3A4 Activity [NCT01361217]		10 participants (Actual)	Interventional	2011-09-30	Completed
Clinical Neuropharmacology of Pain in Spinal Cord Injury- Dextromethorphan/Lidocaine Combination (Factorial Design) Clinical Trial [NCT02218203]	Phase 2	26 participants (Actual)	Interventional	2003-04-30	Completed
Developmental Regulation of CYPs 1A2, 2D6, 3A4 [NCT00117715]		121 participants (Actual)	Observational	2000-10-31	Completed
A Study to Assess Effectiveness, Safety, and Health-related Outcomes of NUEDEXTA® (Dextromethorphan Hydrobromide and Quinidine Sulfate) for the Treatment of Pseudobulbar Affect (PBA) in Nursing Home Patients [NCT02496039]	Phase 4	5 participants (Actual)	Interventional	2015-09-30	Terminated(stopped due to The study was terminated prematurely because of difficulty with recruiting.)
Development of High-throughput Minidose Inje Cocktail Method for Simultaneous Evaluating Five Cytochrome P450 Isoforms in Human [NCT01570569]	Phase 1	26 participants (Actual)	Interventional	2011-01-31	Completed
An Open-Label Tolerance Study of Three Dosing Regimens of Dextromethorphan (DXM) Reportedly Used in Major Depressive Disorder [NCT04226352]	Phase 1	5 participants (Actual)	Interventional	2020-03-15	Completed
A Pilot Study: a Non-opioid Technique for Postoperative Adenoidectomy Pain Relief in Pediatric Patients [NCT03714919]	Phase 2	10 participants (Actual)	Interventional	2019-08-02	Completed
[NCT00004807]		120 participants	Interventional	1995-01-31	Completed
"An Open-label, Single-sequence Study of the Effect of Belatacept on the Pharmacokinetics of Caffeine, Losartan, Omeprazole, Dextromethorphan, and Midazolam Administered as Inje Cocktail in Healthy Subjects" [NCT01766050]	Phase 4	45 participants (Actual)	Interventional	2013-01-31	Completed
A Double-blind, Placebo-controlled, Therapeutic Trial With Antitussive Drug-Dextromethorphan: Aimed to Determine Its Therapeutic Effect in Patients With Rheumatoid Arthritis [NCT02368093]		48 participants (Actual)	Interventional	2010-01-31	Completed
A Phase III Double-Blind Equivalence Study of Two Different Formulations of Slow-Release Morphine Followed by a Randomization Between Dextromethorphan or Placebo Plus Statex SR for Chronic Cancer Pain Relief in Terminally Ill Patients [NCT00003687]	Phase 3	87 participants (Actual)	Interventional	1998-06-11	Completed
A Single Dose, Open Label, Randomized Scintigraphic Study to Investigate the Gastrointestinal Behavior of 2 Triple Combination Products (Acetaminophen, Phenylephrine and Dextromethorphan) in Healthy Male Volunteers [NCT03415243]	Phase 1	28 participants (Actual)	Interventional	2018-03-01	Completed
A Phase 2, Randomized, Double-dummy, Double-blind, Placebo-controlled Study to Assess the Efficacy, Safety and Tolerability of AVP-923 (Dextromethorphan/Quinidine) for the Treatment of Symptoms of Agitation in Patients With Alzheimer's Disease. [NCT01584440]	Phase 2	220 participants (Actual)	Interventional	2012-08-13	Completed
An Open-label Drug Interaction Study in Healthy Subjects to Evaluate the Effect of Oral Doses of JNJ-54175446 on the Inhibition of Cytochrome P450 CYP3A4, CYP2C9, CYP1A2 and CYP2D6 Activity and the Induction of CYP2B6 and CYP2C19 Activity Using a Multiple [NCT03058419]	Phase 1	16 participants (Actual)	Interventional	2017-03-14	Completed
A Randomized Pilot Study of Nuedexta for the Prevention and Modification of Disease Progression in Episodic Migraine [NCT02176018]	Phase 2	76 participants (Actual)	Interventional	2014-08-31	Completed
Glutaminergic and Histaminergic Pathway Modulation in Acute Ischemic Stroke as an Effective Neuroprotection Strategy. [NCT02142712]	Phase 2	3 participants (Actual)	Interventional	2014-12-31	Completed
A Pilot Study Using an NMDA Antagonist to Modulate Transcranial Direct Current Stimulation (tDCS) Effects on Auditory Sensory Memory Processing [NCT02426983]	Phase 1/Phase 2	12 participants (Anticipated)	Interventional	2015-04-30	Not yet recruiting
A Phase I, Open-label, Fixed-sequence, Crossover, Drug-drug Interaction Study to Investigate the Inhibition Potential of KL1333 on CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 in Healthy Subjects [NCT04643249]	Phase 1	14 participants (Actual)	Interventional	2020-11-10	Completed
A Phase 1, Single-center, Randomized, Double-blind, Double-dummy, 2-way Crossover Study Comparing AVP-786 With AVP-923 [NCT02336347]	Phase 1	62 participants (Actual)	Interventional	2014-05-31	Completed
Targeting the NMDA Glutamate Receptor as Novel Antidepressant Strategy: A Pilot Clinical Trial of Nuedexta in Treatment-Resistant Major Depression [NCT01882829]	Phase 2	20 participants (Actual)	Interventional	2013-07-31	Completed
An Open-label Phase 1 Study to Evaluate Drug-Drug Interactions of Agents Co-Administered With Encorafenib and Binimetinib in Patients With BRAF V600-mutant Unresectable or Metastatic Melanoma or Other Advanced Solid Tumors [NCT03864042]	Phase 1	56 participants (Actual)	Interventional	2018-01-02	Active, not recruiting
A Phase I, Open-label, Fixed-sequence, Two-period, Crossover, Drug-drug Interaction Study to Evaluate the Effect of Multiple Doses of Ganaplacide and Lumefantrine Combination on the Pharmacokinetics of Midazolam, Repaglinide, Dextromethorphan, Metformin, [NCT05236530]	Phase 1	48 participants (Actual)	Interventional	2022-03-09	Completed
Clinical Neuropharmacology of Pain in Spinal Cord Injury- Dextromethorphan Dose Response Clinical Trial [NCT01435798]	Phase 2	26 participants (Actual)	Interventional	2003-04-30	Completed
A Pilot Phase I/II Study for the Evaluation of Dextromethorphan as a Microglia Inhibitor in the Treatment of Diabetic Macular Edema (MiDME2) [NCT01441102]	Phase 1/Phase 2	7 participants (Actual)	Interventional	2011-08-31	Completed
Pharmacological Mechanisms of Low-intensity Focused Ultrasound for Motor Cortex Neuroplasticity [NCT04923659]	Early Phase 1	20 participants (Anticipated)	Interventional	2021-05-25	Recruiting
A Randomized Double-blinded Study to Evaluate Preincisional Dextromethorphan in Patients Undergoing Total Knee Arthroplasty and Its Effect on Postoperative Opioid Use [NCT02987920]	Phase 4	23 participants (Actual)	Interventional	2017-01-31	Terminated(stopped due to The surgeon changed pain control protocol for all patients. Continued enrollment impossible under approved protocol.)
Pharmacogenetic Prediction of Metoprolol Effectiveness [NCT02293096]		462 participants (Actual)	Interventional	2014-09-30	Terminated(stopped due to Study was terminated due to the change in funding.)
A Multicenter, Single-Arm, Open-Label Study to Evaluate the Immunogenicity and Pharmacokinetics of BIIB019, Daclizumab High Yield Process (DAC HYP), Prefilled Syringe Administered by Subcutaneous Injection in Subjects With Relapsing-Remitting Multiple Scl [NCT01462318]	Phase 3	133 participants (Actual)	Interventional	2011-11-30	Completed
Effects of Isotretinoin on CYP2D6 Activity [NCT03076021]	Phase 4	36 participants (Actual)	Interventional	2016-07-26	Completed
The Effect of High Dose Rifampicin on the Activity of Cytochrome P450 Enzymes and P-glycoprotein in Patients With Pulmonary Tuberculosis: a Cocktail Phenotyping Study [NCT04525235]	Phase 1	25 participants (Actual)	Interventional	2021-01-07	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00117715 (3) [back to overview]	Change in CYP1A2 Drug Metabolism Phenotype With Age
NCT00117715 (3) [back to overview]	Change in CYP3A4 Drug Metabolism Phenotype With Age
NCT00117715 (3) [back to overview]	Change in CYP2D6 Drug Metabolism Phenotype With Age
NCT00359281 (11) [back to overview]	AUC0-t Simvastatin Acid
NCT00359281 (11) [back to overview]	AUC0-t Nicotinic Acid
NCT00359281 (11) [back to overview]	AUC0-t Nicotinuric Acid
NCT00359281 (11) [back to overview]	AUC0-t Rosuvastatin (Lomitapide 10 mg)
NCT00359281 (11) [back to overview]	AUC0-t Rosuvastatin (Lomitapide 60 mg)
NCT00359281 (11) [back to overview]	Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)
NCT00359281 (11) [back to overview]	AUC0-t Total Ezetimibe
NCT00359281 (11) [back to overview]	AUC0-t Atorvastatin Acid (Lomitapide 60 mg)
NCT00359281 (11) [back to overview]	AUC0-t Fenofibric Acid
NCT00359281 (11) [back to overview]	AUC0-t Simvastatin
NCT00359281 (11) [back to overview]	Area Under Concentration-time Curve From 0 to Last Measureable Concentration (AUC0-t) Atorvastatin Acid (Lomitapide 10 mg)
NCT00377403 (1) [back to overview]	SNOT-16 Score (Sino-Nasal Outcomes Test) at Day 3
NCT00467779 (44) [back to overview]	Stage 1A: MTD of Cobimetinib in 14/14 Schedule
NCT00467779 (44) [back to overview]	Stage 1A: Cmax of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1A: Cmax of Cobimetinib at Cycle 1 Day 1
NCT00467779 (44) [back to overview]	Stage 1A: AUC 0-24 of Cobimetinib at Cycle 1 Day 1
NCT00467779 (44) [back to overview]	Stage 1A: Apparent Clearance of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1A: AUC 0-24/D of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1A: AUC 0-24 of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1A: Accumulation Ratio of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1: Tmax of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1: Time to Maximum Concentration (Tmax) of Cobimetinib at Day 1, Cycle 1
NCT00467779 (44) [back to overview]	Stage 1: Maximum Tolerated Dose (MTD) of Cobimetinib in 21/7 Schedule
NCT00467779 (44) [back to overview]	Stage 1: Maximum Observed Concentration (Cmax) of Cobimetinib at Day 1, Cycle 1
NCT00467779 (44) [back to overview]	Stage 1: Half-Life (t1/2) of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1: Cmax of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1: AUC 0-24/D of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1: AUC 0-24 of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1: Area Under the Plasma Cobimetinib Concentration Curve From Time 0 to 24 Hours (AUC 0-24) Day 1, Cycle 1
NCT00467779 (44) [back to overview]	Stage 1: Apparent Clearance of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1: Accumulation Ratio of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1 and 1A: Number of Participants With Dose Limiting Toxicities (DLTs)
NCT00467779 (44) [back to overview]	Stage 2A: Accumulation Ratio of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2A: Tmax of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2: Accumulation Ratio of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2: Tmax of Cobimetinib at Cycle 1 Day 1
NCT00467779 (44) [back to overview]	Stage 2: Tmax of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2:AUC 0-24 of Cobimetinib at Cycle 1 Day 1
NCT00467779 (44) [back to overview]	Stage 2:Half-Life of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage III: AUC 0-24 of Dextromethorphan
NCT00467779 (44) [back to overview]	Stage 2A: Apparent Clearance of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2A: AUC 0-24/D of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2A: Cmax of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 1A: Tmax of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2A: Half-Life of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage III: Cmax of Dextromethorphan
NCT00467779 (44) [back to overview]	Stage III: AUC0-inf of Midazolam
NCT00467779 (44) [back to overview]	Stage III: AUC0-24 of Midazolam
NCT00467779 (44) [back to overview]	Stage III: AUC 0-inf of Dextromethorphan
NCT00467779 (44) [back to overview]	Stage III: Cmax of Midazolam
NCT00467779 (44) [back to overview]	Stage 2: Apparent Clearance of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2: AUC 0-24 of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2: AUC 0-24/D of Cobimetinib at Steady State
NCT00467779 (44) [back to overview]	Stage 2: Cmax of Cobimetinib at Cycle 1 Day 1
NCT00467779 (44) [back to overview]	Stage 1A: Tmax of Cobimetinib at Cycle 1 Day 1
NCT00467779 (44) [back to overview]	Stage 1A: t1/2 of Cobimetinib at Steady State
NCT00573443 (7) [back to overview]	Mean Change From Baseline at Day 84 in Beck Depression Inventory (BDI-II) Total Score
NCT00573443 (7) [back to overview]	Mean Change From Baseline to Day 84 in Pain Rating Scale (PRS) of MS Subjects
NCT00573443 (7) [back to overview]	Mean Change From Baseline to Day 84 in Neuropsychiatric Inventory (NPI-Q) Frequency and Severity Score (ITT Population)
NCT00573443 (7) [back to overview]	Mean Change From Baseline to Day 84 in Neuropsychiatric Inventory (NPI-Q) Frequency and Severity Score (EE Population)
NCT00573443 (7) [back to overview]	Mean Change From Baseline in CNS-LS Total Score by Visit
NCT00573443 (7) [back to overview]	Mean Change From Baseline at Day 84 in SF-36 (Short-Form) Health Survey Medical Outcome Score by Category
NCT00573443 (7) [back to overview]	PBA Episode Rate Ratio (Post/Pre), Regression Adjusted
NCT00593957 (4) [back to overview]	Difference in EEG Spike Counts at Six Months Compared to Baseline for Each Treatment Arm.
NCT00593957 (4) [back to overview]	Mean SSI Score for Total Subjects at Baseline and 6 Months
NCT00593957 (4) [back to overview]	Improvement in Receptive Language as Measured by the Mullen Scale.
NCT00593957 (4) [back to overview]	Difference in SSI Mean Score at Six Months Compared to Baseline for Each Treatment Arm.
NCT00741468 (1) [back to overview]	Plasma AUC Ratio of Day 1 and Day 8
NCT00873366 (16) [back to overview]	Median of 3 Month Tamoxifen Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]	Median of 3 Month N-desmethyl-tamoxifen (NDMT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]	Median of 3 Month Endoxifen Steady State Concentrations (Endx Css) According to CYP2D6 Phenotype Group and Activity Score
NCT00873366 (16) [back to overview]	Median of 3 Month 4-hydroxy-tamoxifen (4HT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]	Median of 6 Month 4-hydroxy-tamoxifen (4HT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]	Median of 6 Month Endoxifen Steady State Concentrations (Endx Css) According to CYP2D6 Phenotype Group and Activity Score
NCT00873366 (16) [back to overview]	Median of 6 Month N-desmethyl-tamoxifen (NDMT) Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]	Median of 6 Month Tamoxifen Steady State Plasma Concentrations According to CYP2D6 Phenotype Group
NCT00873366 (16) [back to overview]	Operating Characteristics of the ¹³C-dextromethorphan (13C-DM) Breath Test in Identifying Those Who Are CYP2D6 Genotypic Poor Metabolizers
NCT00873366 (16) [back to overview]	Spearman's Rank Correlation Coefficient Between CYP2D6 Activity Score and Endoxifen Steady State Concentrations (Endx Css)
NCT00873366 (16) [back to overview]	Spearman's Rank Correlation Coefficient Between CYP2D6 Activity Score and Endoxifen/N-desmethyl-tamoxifen (Endx/NDMT) Ratio
NCT00873366 (16) [back to overview]	Spearman's Rank Correlation Coefficient Between CYP2D6 Genotype and ¹³Cdextromethorphan Breath Test (DM-BT)
NCT00873366 (16) [back to overview]	Spearman's Rank Correlation Coefficient Between Baseline DM-BT and 3 Month Endoxifen/N-desmethyl-tamoxifen (Endx/NDMT) Ratio
NCT00873366 (16) [back to overview]	Spearman's Rank Correlation Coefficient Between 6 Month DM-BT and 6 Month Endoxifen Steady State Concentrations
NCT00873366 (16) [back to overview]	Spearman's Rank Correlation Coefficient Between 3 Month DM-BT and 3 Month Endoxifen Steady State Concentrations
NCT00873366 (16) [back to overview]	Spearman's Rank Correlation Coefficient Between Baseline DM-BT and 3 Month Endoxifen Steady State Concentrations
NCT01257542 (7) [back to overview]	Change From Baseline in Perceived Numerical Cough Severity Scale for 6 Hour Post-Dose Period
NCT01257542 (7) [back to overview]	Change From Baseline in Perceived Verbal Cough Severity Scale for 6 Hour Post-Dose Period
NCT01257542 (7) [back to overview]	Participants' Global Assessment of Cough: Cough Severity
NCT01257542 (7) [back to overview]	Participants' Global Assessment of Cough: Relief From Cough
NCT01257542 (7) [back to overview]	Total Cough Count
NCT01257542 (7) [back to overview]	Change From Baseline in Verbal Cough Severity Scale at Hours 1, 2, 3, 4, 5 and 6
NCT01257542 (7) [back to overview]	Change From Baseline in Numerical Cough Severity Scale at Hours 1, 2, 3, 4, 5 and 6
NCT01324232 (12) [back to overview]	Average Logarithms of Dextromethorphan (DM) Plasma Concentrations (Cmax) on Days 22 and 50
NCT01324232 (12) [back to overview]	Mean Change From Baseline in Pittsburgh Sleep Quality Index (PSQI) Scores at Day 85
NCT01324232 (12) [back to overview]	Mean Overall Patient Global Impression of Change (PGIC) Scores at Day 85
NCT01324232 (12) [back to overview]	Mean Change From Baseline in Expanded Disability Status Scale (EDSS) Scores at Days 22 and 85
NCT01324232 (12) [back to overview]	Association Between the Dextromethorphan Plasma Concentration and the Change From Baseline Pain Rating Scale (PRS) Score to the Average Pain Rating Scale Score During Days 57 Through 84
NCT01324232 (12) [back to overview]	Comparison of the Adjusted Mean Change From Baseline PRS Score to the Average PRS Score During Days 57 Through 84
NCT01324232 (12) [back to overview]	Mean Change From Baseline in Beck Depression Inventory (BDI-II) Scores at Day 85
NCT01324232 (12) [back to overview]	Mean Change From Baseline in Fatigue Severity Scale (FSS) Scores at Days 57 Through 84
NCT01324232 (12) [back to overview]	Mean Change From Baseline in MS Neuropsychological Screening Questionnaire (MSNQ) Scores at Day 85
NCT01324232 (12) [back to overview]	Mean Change From Baseline in Multiple Sclerosis Impact Scale-29 (MSIS-29) Scores at Day 85
NCT01324232 (12) [back to overview]	Mean Change From Baseline in Symbol Digit Modalities Test (SDMT) Scores at Day 85
NCT01324232 (12) [back to overview]	Mean Numerical Rating Scale (NRS) Scores at Days 22, 50, and 85
NCT01361217 (2) [back to overview]	AUC of Dextromethorphan, Midazolam and Omeprazole in the Presence of Fluoxetine
NCT01361217 (2) [back to overview]	Lovastatin AUC in the Presence of Fluoxetine
NCT01435798 (1) [back to overview]	Mean Pain Intensity (Percent Change From Baseline)
NCT01441102 (17) [back to overview]	Changes in Mean Macular Sensitivity in the Study Eye at 24 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Number of Participants Withdrawn From the Study Therapy Due to Vision Loss or Adverse Events
NCT01441102 (17) [back to overview]	Number of Study Eyes Demonstrating a Decrease in the Area of Late Leakage, as Measured by Fluorescein Angiography (FA), at 12 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Changes in Mean Macular Sensitivity in the Study Eye at 6 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Change in Best-corrected Visual Acuity (BCVA) in the Study Eye at 18 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Change in Best-corrected Visual Acuity (BCVA) in the Study Eye at 24 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Change in Best-corrected Visual Acuity (BCVA) in the Study Eye at 6 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Changes in Mean Macular Sensitivity in the Study Eye at 12 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Change in Best-corrected Visual Acuity (BCVA) in the Study Eye at 12 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Changes in Mean Macular Sensitivity in the Study Eye at 18 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Number of Study Eyes Demonstrating a Decrease in the Area of Late Leakage, as Measured by Fluorescein Angiography (FA), at 18 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Number of Study Eyes Demonstrating a Decrease in the Area of Late Leakage, as Measured by Fluorescein Angiography (FA), at 24 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Number of Study Eyes Demonstrating a Decrease in the Area of Late Leakage, as Measured by Fluorescein Angiography (FA), at 6 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Percentage Change in Retinal Thickness in the Study Eye at 12 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Percentage Change in Retinal Thickness in the Study Eye at 18 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Percentage Change in Retinal Thickness in the Study Eye at 24 Months Compared to Baseline
NCT01441102 (17) [back to overview]	Percentage Change in Retinal Thickness in the Study Eye at 6 Months Compared to Baseline
NCT01462318 (14) [back to overview]	TP-DI Sub-study: Dextromethorphan to Dextrorphan Urine Concentration Ratio
NCT01462318 (14) [back to overview]	TP-DI Sub-study: Omeprazole/Hydroxyomeprazole Concentration Ratio at 2 Hours Post-omeprazole Dosing
NCT01462318 (14) [back to overview]	Intensive PK Sub-study: Apparent Clearance (CL/F) of DAC HYP
NCT01462318 (14) [back to overview]	Intensive PK Sub-study: Apparent Volume of Distribution (V/F) of DAC HYP
NCT01462318 (14) [back to overview]	Intensive PK Sub-study: Elimination Half-life (t½) of DAC HYP
NCT01462318 (14) [back to overview]	Intensive PK Sub-study: Minimum Concentrations (Cmin) of DAC HYP
NCT01462318 (14) [back to overview]	Intensive PK Sub-study: Area-Under-the-Curve From Start to End of the Dosing Interval (AUCtau) of DAC HYP
NCT01462318 (14) [back to overview]	Intensive PK Sub-study: Cmax of DAC HYP
NCT01462318 (14) [back to overview]	Intensive PK Sub-study: Time to Reach Maximum Concentration (Tmax) of DAC HYP
NCT01462318 (14) [back to overview]	Number of Participants With Anti-DAC HYP Binding Antibodies (ADAbs): Electrochemiluminescent (ECL) Anti-Drug Antibody (ADA) Assay
NCT01462318 (14) [back to overview]	Number of Participants With Anti-DAC HYP Neutralizing Antibodies (NAbs): ECL ADA Assay
NCT01462318 (14) [back to overview]	TP-DI Sub-study: Area-Under-the-Curve From Zero to Infinity (AUCinf) of Each Probe Drug
NCT01462318 (14) [back to overview]	TP-DI Sub-study: CL/F of Each Probe Drug
NCT01462318 (14) [back to overview]	TP-DI Sub-study: Cmax of Each Probe Drug
NCT01520363 (17) [back to overview]	Change in PedsQL Social Functioning Subscale Score, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in PedsQL Total Score, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in Rett Syndrome Behavior Questionnaire Score, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in Seizure Frequency, Pre- and Post-Intervention, 0-4 Year Age Group
NCT01520363 (17) [back to overview]	Change in Seizure Frequency, Pre-and Post-Intervention, 5-10 Year Age Group
NCT01520363 (17) [back to overview]	Change in VABS: Socialization Domain Scores, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in VABS: Motor Skills Domain Scores, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in VABS:Communication Domain Scores, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in PedsQL Emotional Functioning Subscale Score, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in VABS:Daily Living Skills Domain Scores, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in Ghuman-Folstein Screen for Social Interaction (SSI) Score, Pre- and Post-Intervention.
NCT01520363 (17) [back to overview]	Change in Mullen, Expressive Language Sub-scale Scores, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in Mullen; Fine Motor Sub-scale Scores, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in Mullen; Receptive Language Subscale Scores, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in Mullen; Visual Reception Sub-scale Scores, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in PedsQL Physical Functioning Subscale Score, Pre- and Post-Intervention
NCT01520363 (17) [back to overview]	Change in PedsQL School Functioning Subscale Score, Pre- and Post-Intervention
NCT01584440 (22) [back to overview]	Number of Participants With the Indicated Change in the Concomitant Use of Allowed Psychotropic Drugs Compared to Their Baseline Use
NCT01584440 (22) [back to overview]	Change in the Caregiver Strain Index (CSI) Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the NPI Agitation/Aggression Domain Score From Day 1 (Stage 1 Baseline) to Day 8 and Day 22 and From Day 36 (Stage 2 Baseline) to Day 43 and Day 57
NCT01584440 (22) [back to overview]	Change in the Alzheimer's Disease Cooperative Study-Activities of Daily Living Inventory (ADCS-ADL) Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the Cornell Scale for Depression in Dementia (CSDD) Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the Individual NPI Domain Scores From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the Mini-Mental State Examination (MMSE) Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline), as Analyzed by the Specified SPCD Methodology
NCT01584440 (22) [back to overview]	Change in the Neuropsychiatric Inventory (NPI) Agitation/Aggression Domain Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the NPI-CDS for the Agitation/Aggression Domain From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the NPI-CDS NPI4A Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the NPI-CDS NPI4D Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the Quality of Life-Alzheimer's Disease (QoL-AD) Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the Sum of the Agitation/Aggression, Irritability/Lability, Anxiety, and Aberrant Motor Behavior NPI Domain (NPI4A) Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the Sum of the Agitation/Aggression, Irritability/Lability, Disinhibition, and Aberrant Motor Behavior NPI Domain (NPI4D) Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the Total Neuropsychiatric Inventory-Caregiver Distress Score (NPI-CDS) From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Change in the Total NPI Score From Day 1 (Stage 1 Baseline) to Day 36 (Stage 2 Baseline) and From Day 36 to Day 70
NCT01584440 (22) [back to overview]	Number of Participants Using Rescue Medications
NCT01584440 (22) [back to overview]	Number of Participants With the Indicated Categorical Response on the Patient Global Impression of Change (PGI-C) for the Caregiver Domain at Day 36 (Stage 2 Baseline) and Day 70 Compared to Their Response at Day 1 (Stage 1 Baseline)
NCT01584440 (22) [back to overview]	Number of Participants With the Indicated Categorical Response on the PGI-C for the Caregiver Domain at Day 70 Compared to Their Response at Day 1 (Stage 1 Baseline)
NCT01584440 (22) [back to overview]	Number of Participants With the Indicated Response on the Alzheimer's Disease Cooperative Study-Clinical Global Impression of Change Rating (mADCS-CGIC) Scale Agitation Domain at Day 36 and Day 70 Compared to Their Response at Day 1 (Stage 1 Baseline)
NCT01584440 (22) [back to overview]	Number of Participants With the Indicated Response on the mADCS-CGIC Scale Agitation Domain at Day 70 Compared to Their Response at Day 36 (Stage 2 Baseline)
NCT01584440 (22) [back to overview]	Number of Participants With the Indicated Type of Adverse Event
NCT01630811 (3) [back to overview]	Primary Safety Endpoints
NCT01630811 (3) [back to overview]	Change in Maladaptive Behaviors
NCT01630811 (3) [back to overview]	Change in Aggressive Behavior
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean Cmax of Dextromethorphan With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean Cmax of Caffeine With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Mean Change From Baseline in Sitting Heart Rate - All Treated Participants
NCT01766050 (36) [back to overview]	Cmax of Inje Cocktail Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	AUC(INF) of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean Area Under the Concentration Time Curve (AUC) From Zero to Last Concentration (0-T) and AUC Extrapolated to Infinity (INF) of Midazolam With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]	Apparent Total Body Clearance (CLT/F) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Number of Participants With Marked Hematology and Urinalysis Laboratory Abnormalities - All Treated Participants
NCT01766050 (36) [back to overview]	Number of Participants With Marked Serum Chemistry Laboratory Abnormalities - All Treated Participants
NCT01766050 (36) [back to overview]	Number of Participants With Out-of-Range Electrocardiogram Intervals - All Treated Participants
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Omeprazole With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Losartan With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]	AUC(0-T) of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Plasma Half-Life (T-HALF) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan, and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Dextromethorphan With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of 1'-Hydroxy-Midazolam AUC(0-T) to Midazolam AUC(0-T) and 1'-Hydroxy-Midazolam AUC(INF) to Midazolam AUC(INF), Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of Paraxanthine (Cmax) to Caffeine (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of E-3174 (Cmax) to Losartan (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of 5-Hydroxyomeprazole (Cmax) to Omeprazole (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of 5-Dextrorphan (Cmax) to Dextromethorphan (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of 5-Dextrorphan AUC(0-T) to Dextromethorphan AUC(0-T) and 5-Dextrorphan AUC(INF) to Dextromethorphan AUC(INF), Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of 5-Hydroxyomeprazole AUC(0-T) to Omeprazole AUC(0-T) and 5-Hydroxyomeprazole AUC(INF) to Omeprazole AUC(INF) , Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC(INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of E-3174 AUC(0-T) to Losartan AUC(0-T) and E3174 AUC (INF) to Losartan AUC (INF) Corrected for Molecular Weight [MR_AUC(0-T), MR_AUC(INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of Paraxanthine AUC(0-T) to Caffeine AUC(0-T) and Paraxanthine AUC (INF) to Caffeine AUC (INF), Corrected for Molecular Weight [MR_AUC(0-T) and MR_AUC (INF)] With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	T-HALF of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Time of Maximum Observed Plasma Concentration (Tmax) of the Inje Cocktail Components (Midazolam, Losartan, Omeprazole, Dextromethorphan, and Caffeine) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Tmax of Inje Cocktail Component Metabolites (1'-Hydroxy-Midazolam, E-3174, 5-Hydroxyomeprazole, Dextrorphan, and Paraxanthine) With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Ratio of 1'-Hydroxy-Midazolam (Cmax) to Midazolam (Cmax), Corrected for Molecular Weight (MR_Cmax) With and Without Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean Cmax of Omeprazole With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]	Mean Change From Baseline in Heart Rate at Study Discharge (Day 46±2 Days)
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean Maximum Drug Concentration (Cmax) of Midazolam With and Without the Coadministration of Belatacept - Pharmacokinetic (PK) Evaluable Population
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean Cmax of Losartan With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01766050 (36) [back to overview]	Mean Change From Baseline in Sitting Systolic and Diastolic Blood Pressure - All Treated Participants
NCT01766050 (36) [back to overview]	Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Study Discharge (Day 46±2 Days)
NCT01766050 (36) [back to overview]	Number of Participants With Adverse Events (AEs), Serious AEs (SAEs), Deaths, and AEs Leading to Discontinuation - All Treated Participants
NCT01766050 (36) [back to overview]	Adjusted Geometric Mean AUC (0-T) and AUC (INF) of Caffeine With and Without the Coadministration of Belatacept - PK Evaluable Population
NCT01767129 (11) [back to overview]	Change From Baseline in the Dyskinesia and Other PD Symptoms Score As Assessed by Patient Global Impression of Change (PGIC)
NCT01767129 (11) [back to overview]	Change From Baseline in MDS-UDysRS Scores for Part 1 and 2
NCT01767129 (11) [back to overview]	"Change From Baseline in PD Motor Diary Ratings Of Duration Of On-time Without Bothersome Dyskinesia"
NCT01767129 (11) [back to overview]	Change From Baseline in PDQ-39 Single Index (PDQ-39-SI) Scores at the End of Each Treatment Period
NCT01767129 (11) [back to overview]	Change From Screening in the Montreal Cognitive Assessment (MoCA) Calculated Score at the End of Each Treatment Period
NCT01767129 (11) [back to overview]	Least Squares Mean Disability Area Under the Curve (AUC) Score As Assessed By Modified Movement Disorder Society-Unified Dyskinesia Rating Scale (MDS-UDysRS) Part 4
NCT01767129 (11) [back to overview]	Least Squares Mean Dyskinesia Severity Area Under the Curve (AUC) Score As Assessed By Modified Movement Disorder Society-Unified Dyskinesia Rating Scale (MDS-UDysRS) Part 3
NCT01767129 (11) [back to overview]	Least Squares Mean Motor Movement Area Under the Curve Score As Assessed by Modified Movement Disorder Society-Unified Parkinson's Disease Rating Scale (MDS-UPDRS), Part III
NCT01767129 (11) [back to overview]	Least Squares Mean Timed Finger Tapping Area Under the Curve (AUC) Score
NCT01767129 (11) [back to overview]	Change From Baseline in MDS-UPDRS Scores for Part I, II, and IV
NCT01767129 (11) [back to overview]	Change From Baseline in Parkinson's Disease Questionnaire-39 (PDQ-39) Domain Scores at the End of Each Treatment Period
NCT01799941 (12) [back to overview]	Percentage of Participants With Clinical Global Impression-Change (CGI-C) Score at Day 90
NCT01799941 (12) [back to overview]	Percentage of Participants With Patient Global Impression-Change (PGI-C) Score at Day 90
NCT01799941 (12) [back to overview]	Percentage of Participants With PBA Remission
NCT01799941 (12) [back to overview]	Percentage of Participants With Treatment Satisfaction Survey
NCT01799941 (12) [back to overview]	Mean Change From Baseline in Center for Neurologic Study-Lability Scale (CNS-LS) Score at Day 30
NCT01799941 (12) [back to overview]	Mean Change From Baseline in Center for Neurologic Study-Lability Scale (CNS-LS) Score at Day 90
NCT01799941 (12) [back to overview]	Mean Change From Baseline in Quality of Life Visual Analog Scale (QOL-VAS) Score at Day 90
NCT01799941 (12) [back to overview]	Mean Pseudobulbar Affect (PBA) Episode Count Per Week by Visit
NCT01799941 (12) [back to overview]	Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT01799941 (12) [back to overview]	Percentage Change From Baseline in PBA Episode Count Per Week
NCT01799941 (12) [back to overview]	Percentage of Participants With ≥ 50% Reduction in PBA Episode Count Per Week
NCT01799941 (12) [back to overview]	Percentage of Participants With ≥ 75% Reduction in PBA Episode Count Per Week
NCT01806857 (16) [back to overview]	Visual Analog Scale - Swallowing Score
NCT01806857 (16) [back to overview]	Average Water Swallowing Test (WST)
NCT01806857 (16) [back to overview]	Average Solids Swallowing Test
NCT01806857 (16) [back to overview]	Ashworth Spasticity Scale Score - Right Leg
NCT01806857 (16) [back to overview]	Ashworth Spasticity Scale Score - Right Arm
NCT01806857 (16) [back to overview]	Ashworth Spasticity Scale Score - Left Leg
NCT01806857 (16) [back to overview]	ALS Functional Rating Scale- Revised (ALSFRS-R) Total Score
NCT01806857 (16) [back to overview]	Ashworth Spasticity Scale Score - Left Arm
NCT01806857 (16) [back to overview]	Visual Analog Scale - Speech Scores
NCT01806857 (16) [back to overview]	Visual Analog Scale - Salivation (Sialorrhea) Score
NCT01806857 (16) [back to overview]	Timed Reading of Test Paragraph Result
NCT01806857 (16) [back to overview]	Center for Neurologic Study - Lability Scale (CNS-LS) Total Score
NCT01806857 (16) [back to overview]	Bulbar Function Scale (CNS-BFS) Total Score
NCT01806857 (16) [back to overview]	Bulbar Function Scale (CNS-BFS) Swallowing Score
NCT01806857 (16) [back to overview]	Bulbar Function Scale (CNS-BFS) Speech Score
NCT01806857 (16) [back to overview]	Bulbar Function Scale (CNS-BFS) Sialorrhea Score
NCT01882829 (11) [back to overview]	Beck Scale for Suicidal Ideation (BSI)
NCT01882829 (11) [back to overview]	Sheehan Disability Scale
NCT01882829 (11) [back to overview]	Range of Impaired Functioning Tool
NCT01882829 (11) [back to overview]	Quick Inventory of Depressive Symptomatology, Self Report (QIDS-SR)
NCT01882829 (11) [back to overview]	Quality of Life Enjoyment and Satisfaction Questionnaire Short Form
NCT01882829 (11) [back to overview]	Patient Rated Inventory of Side Effects (PRISE)
NCT01882829 (11) [back to overview]	Montgomery-Asberg Depression Rating Scale
NCT01882829 (11) [back to overview]	Massachusetts General Hospital Cognitive and Physical Functioning Questionnaire (CPFQ)
NCT01882829 (11) [back to overview]	HAM-A
NCT01882829 (11) [back to overview]	Columbia-Suicide Severity Rating Scale (C-SSRS)
NCT01882829 (11) [back to overview]	Clinical Global Impression (CGI) Scale
NCT02062710 (1) [back to overview]	Change in Cough Reflex Sensitivity to Capsaicin
NCT02142712 (2) [back to overview]	Glasgow Coma Scale (GCS)
NCT02142712 (2) [back to overview]	National Institutes of Health Stroke Severity (NIHSS) Scale
NCT02176018 (10) [back to overview]	Adverse Events
NCT02176018 (10) [back to overview]	Headache Days in Treatment Period Month 3
NCT02176018 (10) [back to overview]	50% Headache Reduction
NCT02176018 (10) [back to overview]	Headache Days in Each Treatment Period Month
NCT02176018 (10) [back to overview]	Headache Duration in Each Treatment Period Month
NCT02176018 (10) [back to overview]	Headache Health Score
NCT02176018 (10) [back to overview]	Headache Severity in Each Treatment Period Month
NCT02176018 (10) [back to overview]	Migraine Days in Each Treatment Period Month
NCT02176018 (10) [back to overview]	Acute Medication Use in Each Treatment Period Month
NCT02176018 (10) [back to overview]	Migraine Disability Assessment Scale (MIDAS)
NCT02218203 (1) [back to overview]	Percent Change in Peak Pain Intensity
NCT02293096 (4) [back to overview]	Adverse Drug Events: CYP2D6 Metabolizer Status
NCT02293096 (4) [back to overview]	Adverse Drug Events: ADRB1 Genotype
NCT02293096 (4) [back to overview]	Heart Rate Decline
NCT02293096 (4) [back to overview]	Blood Pressure Decline
NCT02368093 (1) [back to overview]	Good European League Against Rheumatism (EULAR) Therapeutic Response Rate
NCT02651116 (13) [back to overview]	Mean of Total Cough Counts: Between Dose 1 to Dose 2 on Day 1
NCT02651116 (13) [back to overview]	Mean of Total Cough Counts: Between Dose 2 on Day 1 to Dose 3 on Day 2
NCT02651116 (13) [back to overview]	Mean of Total Cough Counts: Between Dose 3 to Dose 4 on Day 2
NCT02651116 (13) [back to overview]	Mean of Total Cough Time Accumulated Over a 24-Hour Period Post-First Dose on Day 1
NCT02651116 (13) [back to overview]	Change From Baseline in Afternoon Cough Frequency Assessed at Afternoon on Day 2, 3, and 4
NCT02651116 (13) [back to overview]	Change From Baseline in Afternoon Cough Severity Assessed at Afternoon on Day 2, 3, and 4
NCT02651116 (13) [back to overview]	Change From Baseline in Child Global Question Assessed at Afternoon on Day 2, 3, and 4
NCT02651116 (13) [back to overview]	Change From Baseline in Impact of Cough on Sleep Assessed in Morning at Day 2, 3, and 4
NCT02651116 (13) [back to overview]	Change From Baseline in Morning Cough Frequency Assessed in Morning at Day 2, 3, and 4
NCT02651116 (13) [back to overview]	Change From Baseline in Morning Cough Severity Assessed in Morning at Day 2, 3, and 4
NCT02651116 (13) [back to overview]	Pediatric Global Assessment of Satisfaction With Study Medication: By Participant, and Caregiver
NCT02651116 (13) [back to overview]	Mean of Total Cough Counts: Over 24 Hours Post-First Dose on Day 1
NCT02651116 (13) [back to overview]	Mean of Total Cough Counts: Between Dose 1 to Dose 2 on Day 1, and Between Dose 3 to Dose 4 on Day 2
NCT02688088 (14) [back to overview]	Pharmacokinetics: Area Under the Concentration Versus Time Curve [AUC(0-infinity)] of Caffeine
NCT02688088 (14) [back to overview]	Pharmacokinetics: Area Under the Concentration Versus Time Curve [AUC(0-infinity)] of Dextromethorphan
NCT02688088 (14) [back to overview]	Pharmacokinetics: Area Under the Concentration Versus Time Curve [AUC(0-infinity)] of Midazolam
NCT02688088 (14) [back to overview]	Pharmacokinetics: Area Under the Concentration Versus Time Curve [AUC(0-infinity)] of S-Warfarin
NCT02688088 (14) [back to overview]	Mean Change From Baseline at 24 Hours in Pulse Rate in Period 1
NCT02688088 (14) [back to overview]	Pharmacokinetics: Maximum Concentration (Cmax) of Caffeine
NCT02688088 (14) [back to overview]	Pharmacokinetics: Maximum Concentration (Cmax) of Dextromethorphan
NCT02688088 (14) [back to overview]	Pharmacokinetics: Maximum Concentration (Cmax) of Midazolam
NCT02688088 (14) [back to overview]	Mean Change From Baseline at 24 Hours in Pulse Rate in Period 2
NCT02688088 (14) [back to overview]	Pharmacokinetics: Maximum Concentration (Cmax) S-Warfarin
NCT02688088 (14) [back to overview]	Mean Change From Baseline at 24 Hours in Systolic and Diastolic Blood Pressure in Period 1
NCT02688088 (14) [back to overview]	Mean Change From Baseline at 24 Hours in Systolic and Diastolic Blood Pressure in Period 2
NCT02688088 (14) [back to overview]	Mean Change From Baseline at 24 Hours in Systolic and Diastolic Blood Pressure in Period 2
NCT02688088 (14) [back to overview]	Mean Change From Baseline at 24 Hours in Pulse Rate in Period 2
NCT02775240 (33) [back to overview]	Area Under the Plasma Concentration Versus Time Curve From the Time of Dosing to the Last Measurable Concentration (AUClast) of Dextrorphan
NCT02775240 (33) [back to overview]	Area Under the Plasma Concentration Versus Time Curve From the Time of Dosing to the Last Measurable Concentration (AUClast) of Dextromethorphan
NCT02775240 (33) [back to overview]	Area Under the Plasma Concentration Versus Time Curve From the Time of Dosing to the Last Measurable Concentration (AUClast) of Digoxin
NCT02775240 (33) [back to overview]	Apparent Oral Clearance (CL/F) of Digoxin
NCT02775240 (33) [back to overview]	Area Under the Plasma Concentration Versus Time Curve From Time Zero to the End of the Dosing Interval at Steady-State (AUCtau) of Maribavir
NCT02775240 (33) [back to overview]	Concentration at the End of Dosing Interval (Ctau) of Maribavir
NCT02775240 (33) [back to overview]	Apparent Oral Clearance (CL/F) of Maribavir
NCT02775240 (33) [back to overview]	Volume of Distribution Divided by the Fraction of Dose Absorbed (Vz/F) of Dextromethorphan
NCT02775240 (33) [back to overview]	Terminal Half-life (t1/2) of Dextromethorphan
NCT02775240 (33) [back to overview]	Parent/Metabolite Ratio of Area Under the Plasma Concentration Versus Time Curve Extrapolated to Infinity (AUC0-infinity) for Dextromethorphan Over AUC0-infinity for Dextrorphan (AUC0-infinity Parent/Metabolite Ratio)
NCT02775240 (33) [back to overview]	Number of Participants With Study-related Adverse Events (AEs), Serious Adverse Events (SAEs) and Treatment-emergent Adverse Events (TEAEs)
NCT02775240 (33) [back to overview]	First-order Rate Constant (Lambda z) Associated With the Terminal (Log-linear) Portion of the Curve of Dextromethorphan
NCT02775240 (33) [back to overview]	Area Under the Plasma Concentration Versus Time Curve Extrapolated to Infinity (AUC0-infinity) of Dextromethorphan
NCT02775240 (33) [back to overview]	Apparent Oral Clearance (CL/F) of Dextromethorphan
NCT02775240 (33) [back to overview]	Volume of Distribution Divided by the Fraction of Dose Absorbed (Vz/F) of Digoxin
NCT02775240 (33) [back to overview]	Time to Reach Maximum Plasma Concentration (Tmax) of Maribavir
NCT02775240 (33) [back to overview]	Time to Reach Maximum Plasma Concentration (Tmax) of Digoxin
NCT02775240 (33) [back to overview]	Time to Reach Maximum Plasma Concentration (Tmax) of Dextrorphan
NCT02775240 (33) [back to overview]	Time to Reach Maximum Plasma Concentration (Tmax) of Dextromethorphan
NCT02775240 (33) [back to overview]	Terminal Half-life (t1/2) of Maribavir
NCT02775240 (33) [back to overview]	Area Under the Plasma Concentration Versus Time Curve Extrapolated to Infinity (AUC0-infinity) of Dextrorphan
NCT02775240 (33) [back to overview]	Area Under the Plasma Concentration Versus Time Curve Extrapolated to Infinity (AUC0-infinity) of Digoxin
NCT02775240 (33) [back to overview]	Terminal Half-life (t1/2) of Digoxin
NCT02775240 (33) [back to overview]	Number of Participants With Clinically Significant Changes Reported as TEAE in Physical Examination, Vital Signs, 12-lead ECGs, Hematology, Blood Chemistry and Urinalysis
NCT02775240 (33) [back to overview]	First-order Rate Constant (Lambda z) Associated With the Terminal (Log-linear) Portion of the Curve of Dextrorphan
NCT02775240 (33) [back to overview]	First-order Rate Constant (Lambda z) Associated With the Terminal (Log-linear) Portion of the Curve of Digoxin
NCT02775240 (33) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Dextromethorphan
NCT02775240 (33) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Dextrorphan
NCT02775240 (33) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Digoxin
NCT02775240 (33) [back to overview]	Maximum Observed Plasma Concentration (Cmax) of Maribavir
NCT02775240 (33) [back to overview]	Parent/Metabolite Ratio of Area Under the Plasma Concentration Versus Time Curve From the Time of Dosing to the Last Measurable Concentration (AUClast) for Dextromethorphan Over AUClast for Dextrorphan (AUClast Parent/Metabolite Ratio)
NCT02775240 (33) [back to overview]	Pre-dose Concentration (C0) of Maribavir
NCT02775240 (33) [back to overview]	Terminal Half-life (t1/2) of Dextrorphan
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Dextromethorphan
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Omeprazole and Its Metabolite 5-Hydroxyomeprazole
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Omeprazole and Its Metabolite 5-Hydroxyomeprazole
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of Cytochrome P450 (CYP450) Substrate-Midazolam
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Warfarin
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Dextromethorphan
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Maximum Observed Drug Concentration (Cmax) of CYP450 Substrate-Caffeine
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Warfarin
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-∞]) of CYP450 Substrate-Midazolam
NCT02993471 (10) [back to overview]	Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to 48 Hours (AUC[0-48h]) of CYP450 Substrate-Caffeine
NCT03415243 (29) [back to overview]	Small Intestine Transit Time
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 90 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 75 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 60 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 120 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 45 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 30 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 240 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 180 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 15 Minutes of Administration
NCT03415243 (29) [back to overview]	Percentage of Radiolabeled Drug Remaining in the Stomach After 105 Minutes of Administration
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 180 Minutes
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 15 Minutes
NCT03415243 (29) [back to overview]	Mean Time to Onset of Gastric Emptying
NCT03415243 (29) [back to overview]	Mean Time to Complete Gastric Emptying
NCT03415243 (29) [back to overview]	Mean Time for Gastric Emptying by Measuring 90 Percent Values
NCT03415243 (29) [back to overview]	Mean Time for Gastric Emptying by Measuring 50 Percent Values
NCT03415243 (29) [back to overview]	Mean Time for Gastric Emptying by Measuring 25 Percent Values
NCT03415243 (29) [back to overview]	Gastric Emptying Half-Life
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 90 Minutes
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 75 Minutes
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 60 Minutes
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 45 Minutes
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 120 Minutes
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 105 Minutes
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 240 Minutes
NCT03415243 (29) [back to overview]	Total Area Under the Gastric Emptying Curve
NCT03415243 (29) [back to overview]	Area Under the Gastric Emptying Curve From Time 0 to 30 Minutes
NCT03415243 (29) [back to overview]	Number of Participants With Clinically Significant Change in Laboratory Test Values
NCT03471767 (7) [back to overview]	Percentage of Participants Who Experienced a More Than 50% Reduction in Expired Carbon Monoxide (CO) Levels
NCT03471767 (7) [back to overview]	Urinary Levels of Dextromethorphan
NCT03471767 (7) [back to overview]	Change in Smoking Behavior
NCT03471767 (7) [back to overview]	Change in Smoking Intensity
NCT03471767 (7) [back to overview]	Medication Adherence
NCT03471767 (7) [back to overview]	Medication Tolerance by Self-Reported Side Effects
NCT03471767 (7) [back to overview]	Medication Tolerance by Serious Adverse Events
NCT03480009 (4) [back to overview]	Mean Pain Scores Via Numeric Rating Scale (NRS-11)
NCT03480009 (4) [back to overview]	Analgesic Usage During Medication Abortion
NCT03480009 (4) [back to overview]	Analgesic Usage During Medication Abortion
NCT03480009 (4) [back to overview]	Worst Pain Measurement Via Numeric Rating Scale (NRS-11)
NCT03538054 (2) [back to overview]	Daily Self-reported Physical Activity
NCT03538054 (2) [back to overview]	Daily Self-reported Pain Severity
NCT03714919 (5) [back to overview]	Time in PACU
NCT03714919 (5) [back to overview]	Number of Participants With Sedation, Nausea/Vomiting, or Hallucinations
NCT03714919 (5) [back to overview]	Extubation Time
NCT03714919 (5) [back to overview]	End of Surgery to Hospital Discharge
NCT03714919 (5) [back to overview]	Average Pain Score
NCT03883581 (5) [back to overview]	Change in Speech Intelligibility
NCT03883581 (5) [back to overview]	Change in Patient-reported Outcome: Center for Neurologic Study-Bulbar Function Scale (CNS-BFS)
NCT03883581 (5) [back to overview]	Change in Dynamic Imaging Grade of Swallowing Toxicity
NCT03883581 (5) [back to overview]	Change in ALSFRS-R Bulbar Subscale Score
NCT03883581 (5) [back to overview]	Bamboo Passage Reading Duration (in Seconds)
NCT04039022 (1) [back to overview]	Incidence of Treatment-emergent AEs (TEAEs) Following Dosing With AXS-05
NCT04392011 (7) [back to overview]	Midazolam and Dextromethorphan Half-life
NCT04392011 (7) [back to overview]	Mitragynine Area Under the Concentration vs. Time Curve (AUC)
NCT04392011 (7) [back to overview]	Mitragynine Cmax
NCT04392011 (7) [back to overview]	Mitragynine Half Life
NCT04392011 (7) [back to overview]	Midazolam and Dextromethorphan Cmax
NCT04392011 (7) [back to overview]	Dextromethorphan Area Under the Concentration vs. Time Curve (AUC)
NCT04392011 (7) [back to overview]	Midazolam Area Under the Concentration vs. Time Curve (AUC)

Change in CYP1A2 Drug Metabolism Phenotype With Age

Concentrations of caffeine metabolites 5-Acetylamino-6-amino-3-methyluracil (AAMU), 1-methylxanthine (1MX), 1-methyluric acid (1MU), and 1,7-dimethyluric acid (17MU) are quantified in urine and used to estimate the activity of cytochrome P450 1A2 using the well established (AAMU+1MX+1MU)/1,7U ratio. The longitudinal study design allows for changes in drug metabolism activity as a function of age which can be characterized via least squares regression where the slope of age vs. (AAMU+1MX+1MU)/1,7U ratio is examined for deviations from zero. (NCT00117715)
Timeframe: every 6 months for 5 years

Intervention	unitless ratio (Mean)
	Log ((AAMU+1MX+1MU)/1,7U) Milestone 1	Log ((AAMU+1MX+1MU)/1,7U) Milestone 2	Log ((AAMU+1MX+1MU)/1,7U) Milestone 3	Log ((AAMU+1MX+1MU)/1,7U) Milestone 4	Log ((AAMU+1MX+1MU)/1,7U) Milestone 5	Log ((AAMU+1MX+1MU)/1,7U) Milestone 6	Log ((AAMU+1MX+1MU)/1,7U) Milestone 7	Log ((AAMU+1MX+1MU)/1,7U) Milestone 8	Log ((AAMU+1MX+1MU)/1,7U) Milestone 9
Longitudinal Assessment Cohort	-0.851	-0.823	-0.858	-0.856	-0.832	-0.853	-0.822	-0.851	-0.821

Intervention	unitless ratio (Mean)
	Log (3HM/DX) Milestone 1	Log (3HM/DX) Milestone 2	Log (3HM/DX) Milestone 3	Log (3HM/DX) Milestone 4	Log (3HM/DX) Milestone 5	Log (3HM/DX) Milestone 6	Log (3HM/DX) Milestone 7	Log (3HM/DX) Milestone 8	Log (3HM/DX) Milestone 9
Longitudinal Assessment Cohort	-0.069	-0.117	-0.142	-0.158	-0.109	-0.136	-0.133	-0.122	-0.169

Intervention	unitless ratio (Mean)
	Log (DM/DX) Milestone 1	Log (DM/DX) Milestone 2	Log (DM/DX) Milestone 3	Log (DM/DX) Milestone 4	Log (DM/DX) Milestone 5	Log (DM/DX) Milestone 6	Log (DM/DX) Milestone 7	Log (DM/DX) Milestone 8	Log (DM/DX) Milestone 9
Longitudinal Assessment Cohort	-1.974	-2.083	-2.162	-2.073	-2.161	-2.185	-2.284	-2.177	-2.384

Intervention	Percent Change (Mean)
Atorvastatin 20 mg + Lomitapide 10 mg	-30.99
Simvastatin 20 mg + Lomitapide 10 mg	-26.43
Ezetimibe 10 mg + Lomitapide 10 mg	-28.36
Rosuvastatin 20 mg + Lomitapide 10 mg	-41.74
Fenofibrate 145 mg + Lomitapide 10 mg	-20.12
Atorvastatin 20 mg + Lomitapide 60 mg	-66.02
Rosuvastatin 20 mg + Lomitapide 60 mg	-63.20
Dextrometh-rophan 30 mg + Lomitapide 60 mg	-46.07
ER Niacin 1000 mg + Lomitapide 10 mg	-20.89

Intervention	ng/mL (Mean)
Stage 1A Cohort 01A - Cobimetinib 60 mg (14/14)	180.0
Stage 1A Cohort 02A - Cobimetinib 80 mg (14/14)	494.0
Stage 1A Cohort 03A - Cobimetinib 100 mg (14/14)	640.0
Stage 1A Cohort 04A - Cobimetinib 125 mg (14/14)	1160.0

Intervention	ng/mL (Mean)
Stage 1A Cohort 01A - Cobimetinib 60 mg (14/14)	78.4
Stage 1A Cohort 02A - Cobimetinib 80 mg (14/14)	167.0
Stage 1A Cohort 03A - Cobimetinib 100 mg (14/14)	258.0
Stage 1A Cohort 04A - Cobimetinib 125 mg (14/14)	533.0

Intervention	h*ng/mL (Mean)
Stage 1A Cohort 01A - Cobimetinib 60 mg (14/14)	1140
Stage 1A Cohort 02A - Cobimetinib 80 mg (14/14)	2130
Stage 1A Cohort 03A - Cobimetinib 100 mg (14/14)	4020
Stage 1A Cohort 04A - Cobimetinib 125 mg (14/14)	7190

Intervention	L/hr (Mean)
Stage 1A Cohort 01A - Cobimetinib 60 mg (14/14)	25.1
Stage 1A Cohort 02A - Cobimetinib 80 mg (14/14)	14.9
Stage 1A Cohort 03A - Cobimetinib 100 mg (14/14)	21.9
Stage 1A Cohort 04A - Cobimetinib 125 mg (14/14)	6.9

Intervention	ng*hr/mL/mg (Mean)
Stage 1A Cohort 01A - Cobimetinib 60 mg (14/14)	49.8
Stage 1A Cohort 02A - Cobimetinib 80 mg (14/14)	84.2
Stage 1A Cohort 03A - Cobimetinib 100 mg (14/14)	115.0
Stage 1A Cohort 04A - Cobimetinib 125 mg (14/14)	172.0

Intervention	h*ng/mL (Mean)
Stage 1A Cohort 01A - Cobimetinib 60 mg (14/14)	2990.0
Stage 1A Cohort 02A - Cobimetinib 80 mg (14/14)	6740.0
Stage 1A Cohort 03A - Cobimetinib 100 mg (14/14)	11500.0
Stage 1A Cohort 04A - Cobimetinib 125 mg (14/14)	21500.0

Intervention	ratio (Mean)
Stage 1A Cohort 01A - Cobimetinib 60 mg (14/14)	2.32
Stage 1A Cohort 02A - Cobimetinib 80 mg (14/14)	3.14
Stage 1A Cohort 03A - Cobimetinib 100 mg (14/14)	2.6
Stage 1A Cohort 04A - Cobimetinib 125 mg (14/14)	5.15

Intervention	hours (Median)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	4.0
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	1.0
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	2.25
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	4.0
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	3.0
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	2.0
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	3.0
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	2.5

Intervention	ng/mL (Geometric Mean)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	4.51
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	6.92
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	18.3
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	18.8
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	30.8
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	71.7
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	163.0
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	261.0

Intervention	hours (Median)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	80.0
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	64.0
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	47.8
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	66.0
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	50.5
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	41.3
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	51.3
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	60.0

Intervention	ng/mL (Mean)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	13.5
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	19.8
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	28.7
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	53.0
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	54.7
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	341.0
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	401.0
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	641.0

Intervention	ng*hr/mL/mg (Mean)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	62.4
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	34
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	28.2
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	76.3
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	44.3
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	134
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	104
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	132

Intervention	h*ng/mL (Mean)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	202.0
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	288.0
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	411.0
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	763.0
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	886.0
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	5370.0
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	6250.0
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	10500.0

Intervention	h*ng/mL (Geometric Mean)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	56.2
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	68.0
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	203.0
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	242.0
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	440.0
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	785.0
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	1620.0
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	3060.0

Intervention	Liters per hour (L/hr) (Mean)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	22.4
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	34.0
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	37.1
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	13.5
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	22.6
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	14.0
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	11.8
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	11.6

Intervention	ratio (Mean)
Stage 1 Cohort 01 - Cobimetinib 0.05 mg/kg (21/7)	3.56
Stage 1 Cohort 02 - Cobimetinib 0.10 mg/kg (21/7)	3.66
Stage 1 Cohort 03 - Cobimetinib 0.20 mg/kg (21/7)	2.65
Stage 1 Cohort 04 - Cobimetinib 10 mg (21/7)	3.23
Stage 1 Cohort 05 - Cobimetinib 20 mg (21/7)	2.96
Stage 1 Cohort 06 - Cobimetinib 40 mg (21/7)	3.61
Stage 1 Cohort 07 - Cobimetinib 60 mg (21/7)	2.87
Stage 1 Cohort 08 - Cobimetinib 80 mg (21/7)	3.26

Intervention	h*ng/mL (Geometric Mean)
	With cobimetinib - Cycle 1 Day 1 (n=17)	Without cobimetinib - Cycle 1 Day1 (n=19)
Stage 3 Cohort 40 - Cobimetinib+Midazolam+Dextromethorphan	24.8	25.8

dextromethorphan

Description

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Protein Targets (36)

Potency Measurements

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Research Demand Index: 94.02

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Clinical Trials (136)

Trial Overview

Trial Outcomes

Change in CYP1A2 Drug Metabolism Phenotype With Age

Change in CYP3A4 Drug Metabolism Phenotype With Age

Change in CYP2D6 Drug Metabolism Phenotype With Age

AUC0-t Simvastatin Acid

AUC0-t Nicotinic Acid

AUC0-t Nicotinuric Acid

AUC0-t Rosuvastatin (Lomitapide 10 mg)

AUC0-t Rosuvastatin (Lomitapide 60 mg)

Percent Change From Baseline in Low-density Lipoprotein Cholesterol (LDL-C)

AUC0-t Total Ezetimibe

AUC0-t Atorvastatin Acid (Lomitapide 60 mg)

AUC0-t Fenofibric Acid

AUC0-t Simvastatin

Area Under Concentration-time Curve From 0 to Last Measureable Concentration (AUC0-t) Atorvastatin Acid (Lomitapide 10 mg)

SNOT-16 Score (Sino-Nasal Outcomes Test) at Day 3

Stage 1A: MTD of Cobimetinib in 14/14 Schedule

Stage 1A: Cmax of Cobimetinib at Steady State

Stage 1A: Cmax of Cobimetinib at Cycle 1 Day 1

Stage 1A: AUC 0-24 of Cobimetinib at Cycle 1 Day 1

Stage 1A: Apparent Clearance of Cobimetinib at Steady State

Stage 1A: AUC 0-24/D of Cobimetinib at Steady State

Stage 1A: AUC 0-24 of Cobimetinib at Steady State

Stage 1A: Accumulation Ratio of Cobimetinib at Steady State

Stage 1: Tmax of Cobimetinib at Steady State

Stage 1: Time to Maximum Concentration (Tmax) of Cobimetinib at Day 1, Cycle 1

Stage 1: Maximum Tolerated Dose (MTD) of Cobimetinib in 21/7 Schedule

Stage 1: Maximum Observed Concentration (Cmax) of Cobimetinib at Day 1, Cycle 1

Stage 1: Half-Life (t1/2) of Cobimetinib at Steady State

Stage 1: Cmax of Cobimetinib at Steady State

Stage 1: AUC 0-24/D of Cobimetinib at Steady State

Stage 1: AUC 0-24 of Cobimetinib at Steady State

Stage 1: Area Under the Plasma Cobimetinib Concentration Curve From Time 0 to 24 Hours (AUC 0-24) Day 1, Cycle 1

Stage 1: Apparent Clearance of Cobimetinib at Steady State

Stage 1: Accumulation Ratio of Cobimetinib at Steady State

Stage 1 and 1A: Number of Participants With Dose Limiting Toxicities (DLTs)

Stage 2A: Accumulation Ratio of Cobimetinib at Steady State

Stage 2A: Tmax of Cobimetinib at Steady State

Stage 2: Accumulation Ratio of Cobimetinib at Steady State

Stage 2: Tmax of Cobimetinib at Cycle 1 Day 1

Stage 2: Tmax of Cobimetinib at Steady State

Stage 2:AUC 0-24 of Cobimetinib at Cycle 1 Day 1

Stage 2:Half-Life of Cobimetinib at Steady State

Stage III: AUC 0-24 of Dextromethorphan

Stage 2A: Apparent Clearance of Cobimetinib at Steady State

Stage 2A: AUC 0-24/D of Cobimetinib at Steady State

Stage 2A: Cmax of Cobimetinib at Steady State

Intervention	ng/mL (Geometric Mean)
	With cobimetinib - Cycle 1 Day 15(n=17)	Without cobimetinib - Cycle 1 Day 1 (n=20)
Stage 3 Cohort 40 - Cobimetinib+Midazolam+Dextromethorphan	3.44	3.16

Intervention	h*ng/mL (Geometric Mean)
	With cobimetinib - Cycle 1 Day 15 (n=17)	Without cobimetinib Cycle 1 Day 1 (n=19)
Stage 3 Cohort 40 - Cobimetinib+Midazolam+Dextromethorphan	34.9	35.7

Intervention	h*ng/mL (Geometric Mean)
	With cobimetinib - Cycle 1 Day 15 (n=14)	Without cobimetinib - Cycle 1 Day 1 (n=11)
Stage 3 Cohort 40 - Cobimetinib+Midazolam+Dextromethorphan	33.0	33.4

Intervention	h*ng/mL (Geometric Mean)
	With cobimetinib - Cycle 1 Day 15 (n=13)	Without cobimetinib - Cycle 1 Day1 (n=19)
Stage 3 Cohort 40 - Cobimetinib+Midazolam+Dextromethorphan	29.1	18.9

Intervention	ng/mL (Geometric Mean)
	With cobimetinib - Cycle 1 Day15 (n=17)	Without cobimetinib - Cycle 1 Day 1(n=20)
Stage 3 Cohort 40 - Cobimetinib+Midazolam+Dextromethorphan	11.5	10.9

Intervention	hours (Median)
Stage 1A Cohort 01A - Cobimetinib 60 mg (14/14)	59.4
Stage 1A Cohort 02A - Cobimetinib 80 mg (14/14)	44.1
Stage 1A Cohort 03A - Cobimetinib 100 mg (14/14)	51.6
Stage 1A Cohort 04A - Cobimetinib 125 mg (14/14)	47.7

Intervention	Scores on a Scale (Mean)
	Frequency Score	Severity Score
AVP-923-20	-2.56	-1.59
AVP-923-30	-1.62	-0.74
Placebo	-1.33	-0.98

Intervention	Scores on a Scale (Mean)
	Day 15 (Visit2)	Day 29 (Visit 3)	Day 57 (Visit 4)	Day 84 (Visit 5)
AVP-923-20	-6.27	-7.62	-8.89	-8.24
AVP-923-30	-6.77	-8.03	-8.59	-8.17
Placebo	-4.58	-5.70	-5.66	-5.72

Intervention	Scores on a Scale (Mean)
	Physical Functioning Scale	Role Physical Scale	Bodily Pain Scale	General Health Scale	Vitality Scale	Social Functioning Scale	Role Emotional Scale	Mental Health Scale
AVP-923-20	-5.30	-4.26	5.84	-2.95	-5.30	1.42	-1.81	3.09
AVP-923-30	-0.90	3.47	4.09	-1.47	-0.90	9.34	11.55	5.53
Placebo	-4.05	-1.75	-1.13	-1.28	-4.05	-3.09	2.36	-0.28

Intervention	EEG spike counts per minute (Mean)
Dextromethorphan (DM)1 EEG Spike Counts at Baseline	44.22
DM2 EEG Spike Counts at Baseline	25.44
DM3 EEG Spike Counts at Baseline	40.67
DM1 EEG Spike Count at 6 Months	38.29
DM2 EEG Spike Counts at 6 Months	27.58
DM3 EEG Spike Counts at 6 Months	36.01