cenicriviroc profile

cenicriviroc: an inhibitor of HIV-1 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cenicriviroc : A member of the class of benzazocines that is (5Z)-1,2,3,4-tetrahydro-1-benzazocine which is substituted by a 2-methylpropyl, N-{4-[(S)-(1-propyl-1H-imidazol-5-yl)methanesulfinyl]phenyl}carboxamide and 4-(2-butoxyethoxy)phenyl groups at positions 1, 5 and 8, respectively. It is a potent chemokine 2 and 5 receptor antagonist currently in development for the treatment of liver fibrosis in adults with nonalcoholic steatohepatitis (NASH). [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	11285792
CHEMBL ID	2110727
CHEBI ID	149636
SCHEMBL ID	3157768
SCHEMBL ID	3157748
MeSH ID	M0493908

Synonym
(5e)-8-[4-(2-butoxyethoxy)phenyl]-1-(2-methylpropyl)-n-[4-[(s)-(3-propylimidazol-4-yl)methylsulfinyl]phenyl]-3,4-dihydro-2h-1-benzazocine-5-carboxamide
tak 652
tak-652
tak652
tbr652
cenicriviroc
1-benzazocine-5-carboxamide, 8-[4-(2-butoxyethoxy)phenyl]-1,2,3,4-tetrahydro-1-(2-methylpropyl)-n-[4-[[(1-propyl-1h-imidazol-5-yl)methyl]sulfinyl]phenyl]-, (5e)-
(5e)-8-[4-(2-butoxyethoxy)phenyl]-1-isobutyl-n-[4-[(s)-(3-propylimidazol-4-yl)methylsulfinyl]phenyl]-3,4-dihydro-2h-1-benzazocine-5-carboxamide
tbr-652
bdbm50306033
CVC ,
CHEBI:149636
cenicrivirocum
497223-25-3
(5e)-8-[4-(2-butoxyethoxy)phenyl]-1-(2-methylpropyl)-n-(4-{(s)-[(1-propyl-1h-imidazol-5-yl)methyl]sulfinyl}phenyl)-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide
tbr 652
D09878
cenicriviroc (usan/inn)
CHEMBL2110727
cenicriviroc [usan:inn]
(-)-8-(4-(2-butoxyethoxy)phenyl)-1-isobutyl-n-(4-(((1-propyl-1h-imidazol-5-yl)methyl)sulfinyl)phenyl)-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide
15c116ua4y ,
1-benzazocine-5-carboxamide, 8-(4-(2-butoxyethoxy)phenyl)-1,2,3,4-tetrahydro-1-(2-methylpropyl)-n-(4-((s)-((1-propyl-1h-imidazol-5-yl)methyl)sulfinyl)phenyl)-
8-(4-(2-butoxyethoxy)phenyl)-1,2,3,4-tetrahydro-1-(2-methylpropyl)-n-(4-((s)-((1-propyl-1h-imidazol-5-yl)methyl)sulfinyl)phenyl)-1-benzazocine-5-carboxamide
unii-15c116ua4y
S8512
bdbm50422828
cenicriviroc [usan]
8-(4-(2-(butoxy)ethoxy)phenyl)-1-(2-methylpropyl)-n-(4-((s)-((1-propyl-1h-imidazol-5-yl)methyl)sulfinyl)phenyl)-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide
(s)-8-(4-(2-butoxyethoxy)phenyl)-1-(2-methylpropyl)-n-(4-(((1-propyl-1h-imidazol-5- yl)methyl)sulfinyl)phenyl)-1,2,3,4-tetrahydro-1-benzazocine-5-carboxamide
1-benzazocine-5-carboxamide, 8-(4-(2-butoxyethoxy)phenyl)-1,2,3,4-tetrahydro-1-(2- methylpropyl)-n-(4-((s)-((1-propyl-1h-imidazol-5-yl)methyl)sulfinyl)phenyl)-
cenicriviroc [inn]
cenicriviroc [who-dd]
SCHEMBL3157768
SCHEMBL3157748
AC-31368
CS-6148
HY-14882
AKOS027250788
mfcd28502076
DB11758
(s,e)-8-(4-(2-butoxyethoxy)phenyl)-1-isobutyl-n-(4-(((1-propyl-1h-imidazol-5-yl)methyl)sulfinyl)phenyl)-1,2,3,4-tetrahydrobenzo[b]azocine-5-carboxamide
EX-A1608
AS-35184
Q5058846
AMY12051
tak-652; tbr-652
497223-25-3 (free base)
tbr-652tak-652
BC179068

Excerpt	Reference
"Cenicriviroc (CVC) is a novel, orally administered, potent chemokine 2 and 5 receptor antagonist currently in development for the treatment of liver fibrosis in adults with NASH."	( Cenicriviroc for the treatment of liver fibrosis in adults with nonalcoholic steatohepatitis: AURORA Phase 3 study design. Abdelmalek, MF; Alkhouri, N; Anstee, QM; Bedossa, P; Fischer, L; Goodman, Z; Neuschwander-Tetri, BA; Pecoraro, ML; Sanyal, A; Seyedkazemi, S; Tacke, F; Wong, VW; Younossi, ZM; Yuan, J, 2020)
"Cenicriviroc (CVC) is a C-C chemokine receptors type 2 and 5 dual antagonist under evaluation for treating liver fibrosis in adults with nonalcoholic steatohepatitis (NASH). "	( Cenicriviroc Treatment for Adults With Nonalcoholic Steatohepatitis and Fibrosis: Final Analysis of the Phase 2b CENTAUR Study. Abdelmalek, MF; Aithal, GP; Fischer, L; Francque, S; Goodman, Z; Harrison, SA; Kowdley, KV; Loomba, R; Ratziu, V; Sanyal, A; Seyedkazemi, S; Tacke, F; Wong, VW, 2020)
"Cenicriviroc (CVC) is a small-molecule chemokine receptor antagonist with highly potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity through antagonizing C-C chemokine receptor type 5 (CCR5) as a coreceptor of HIV-1. "	( The chemokine receptor antagonist cenicriviroc inhibits the replication of SARS-CoV-2 in vitro. Baba, M; Okamoto, M; Toyama, M, 2020)
"Cenicriviroc is an oral inhibitor of the chemokine ligand 2/C-C chemokine receptor 2 pathway, which plays an important role in the hepatic recruitment of the macrophages."	( Role of cenicriviroc in the management of nonalcoholic fatty liver disease. Neokosmidis, G; Tziomalos, K, 2018)
"Cenicriviroc is a potent antagonist of the chemokine coreceptors 5 and 2 (CCR5/CCR2) and blocks HIV-1 entry. "	( The dual CCR5 and CCR2 inhibitor cenicriviroc does not redistribute HIV into extracellular space: implications for plasma viral load and intracellular DNA decline. Colby-Germinario, SP; Hassounah, S; Kramer, VG; Lefebvre, E; Mesplède, T; Oliveira, M; Wainberg, MA, 2015)
"Cenicriviroc is a CCR5 antagonist which prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry. "	( Incompatible Natures of the HIV-1 Envelope in Resistance to the CCR5 Antagonist Cenicriviroc and to Neutralizing Antibodies. Baba, M; Enomoto, I; Kuwata, T; Matsushita, S, 2016)
"Cenicriviroc (CVC) is an oral, dual CCR2/CCR5 antagonist with nanomolar potency against both receptors."	( Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis. Chou, HL; Friedman, SL; Hashiguchi, T; Hong, F; Jenkins, H; Lefebvre, E; Moyle, G; Plato, C; Poulin, D; Reshef, R; Richards, T; Richman, LP; Thompson, M; Wolfgang, G; Yoneyama, H, 2016)
"Cenicriviroc is a promising CCR5 inhibitor with potentially important anti-inflammatory effects, and warrants further investigation."	( Cenicriviroc, an orally active CCR5 antagonist for the potential treatment of HIV infection. Iler, CA; Klibanov, OM; Williams, SH, 2010)

Excerpt	Reference
"Cenicriviroc treatment of HAoECs alone decreased monocyte migration in the HIV-infected group when compared to vehicle (P < 0.01)."	( Cenicriviroc inhibits trans-endothelial passage of monocytes and is associated with impaired E-selectin expression. Baumer, Y; Boisvert, WA; Byron, MM; Chow, D; D'Antoni, ML; Lefebvre, E; McCurdy, S; Mehta, NN; Mitchell, BI; Ndhlovu, LC; Ogata-Arakaki, D; Shikuma, CM, 2018)

Excerpt	Reference
" Laboratory and clinical adverse events (AEs) and electrocardiogram changes were recorded."	( Safety, efficacy, and pharmacokinetics of TBR-652, a CCR5/CCR2 antagonist, in HIV-1-infected, treatment-experienced, CCR5 antagonist-naive subjects. Brinson, C; Cohen, C; Dejesus, E; Ernst, JA; Galindez, J; Gathe, J; Lalezari, J; Martin, DE; Palleja, SM; Thompson, M, 2011)
" TBR-652 was generally safe and well tolerated, with no withdrawals due to AEs."	( Safety, efficacy, and pharmacokinetics of TBR-652, a CCR5/CCR2 antagonist, in HIV-1-infected, treatment-experienced, CCR5 antagonist-naive subjects. Brinson, C; Cohen, C; Dejesus, E; Ernst, JA; Galindez, J; Gathe, J; Lalezari, J; Martin, DE; Palleja, SM; Thompson, M, 2011)
" No network meta-analysis (NMA) analyzes the adverse events of antifibrotic drugs for NAFLD."	( Side effect profile of pharmacologic therapies for liver fibrosis in nonalcoholic fatty liver disease: a systematic review and network meta-analysis. Feng, P; Lei, H; Lei, R; Li, Y; Xie, F; Xiong, Q; Yao, C, 2023)

Excerpt	Reference
" Pharmacokinetic data were analyzed using noncompartmental statistics."	( Safety, efficacy, and pharmacokinetics of TBR-652, a CCR5/CCR2 antagonist, in HIV-1-infected, treatment-experienced, CCR5 antagonist-naive subjects. Brinson, C; Cohen, C; Dejesus, E; Ernst, JA; Galindez, J; Gathe, J; Lalezari, J; Martin, DE; Palleja, SM; Thompson, M, 2011)
" As it is metabolized by the liver, cenicriviroc was investigated in hepatic-impaired participants for pharmacokinetic changes."	( Pharmacokinetics, Safety, and CCR2/CCR5 Antagonist Activity of Cenicriviroc in Participants With Mild or Moderate Hepatic Impairment. Chang, W; Gottwald, M; Lasseter, K; Lefebvre, E; Smith, PF; Somasunderam, A; Utay, NS; Willett, M, 2016)

Excerpt	Reference
" TAK-652 is an orally bioavailable TAK-779 derivative with potent anti-HIV-1 activity."	( TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans. Baba, M; Iizawa, Y; Kanzaki, N; Miyake, H; Shiraishi, M; Takashima, K; Teshima, K; Wang, X, 2005)
"Chemical modification has been performed on an orally bioavailable and potent CCR5 antagonist, sulfoxide compound 4, mainly focusing on replacement of the [6,7]-fused 1-benzazepine nucleus."	( Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. Aikawa, K; Aramaki, Y; Baba, M; Iizawa, Y; Kanzaki, N; Kuze, Y; Miyamoto, N; Seto, M; Shiraishi, M; Takashima, K, 2006)
" Since TAK-652 is orally bioavailable and has favorable pharmacokinetic profiles in humans, it is considered a promising candidate for an entry inhibitor of HIV-1."	( Isolation and characterization of human immunodeficiency virus type 1 resistant to the small-molecule CCR5 antagonist TAK-652. Baba, M; Miyake, H; Okamoto, M; Takashima, K; Wang, X, 2007)

Role	Description
chemokine receptor 5 antagonist	An antogonist that blocks chemokine receptor 5 (CCR5).
anti-HIV agent	An antiviral agent that destroys or inhibits the replication of the human immunodeficiency virus.
chemokine receptor 2 antagonist	An antogonist that blocks chemokine receptor 2 (CCR2).
antirheumatic drug	A drug used to treat rheumatoid arthritis.
anti-inflammatory agent	Any compound that has anti-inflammatory effects.
[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
diether	A polyether in which the number of ether linkages is 2.
imidazoles	A five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
sulfoxide	An organosulfur compound having the structure R2S=O or R2C=S=O (R =/= H).
aromatic ether	Any ether in which the oxygen is attached to at least one aryl substituent.
secondary carboxamide	A carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
benzazocine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
C-C chemokine receptor type 7	Homo sapiens (human)	IC50 (µMol)	0.0031	0.0014	0.0023	0.0031	AID1546906
C-C chemokine receptor type 2	Homo sapiens (human)	IC50 (µMol)	0.0059	0.0000	0.6736	6.6990	AID1546905; AID707915
C-C chemokine receptor type 5	Homo sapiens (human)	IC50 (µMol)	0.0030	0.0002	0.2567	9.0000	AID707914
C-C chemokine receptor type 5	Mus musculus (house mouse)	IC50 (µMol)	0.0003	0.0003	0.0017	0.0052	AID1353545
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
negative regulation of interleukin-12 production	C-C chemokine receptor type 7	Homo sapiens (human)
establishment of T cell polarity	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of cell-matrix adhesion	C-C chemokine receptor type 7	Homo sapiens (human)
dendritic cell chemotaxis	C-C chemokine receptor type 7	Homo sapiens (human)
myeloid dendritic cell chemotaxis	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of dendritic cell antigen processing and presentation	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of hypersensitivity	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of humoral immune response	C-C chemokine receptor type 7	Homo sapiens (human)
inflammatory response	C-C chemokine receptor type 7	Homo sapiens (human)
G protein-coupled receptor signaling pathway	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of actin filament polymerization	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of pseudopodium assembly	C-C chemokine receptor type 7	Homo sapiens (human)
ruffle organization	C-C chemokine receptor type 7	Homo sapiens (human)
response to lipopolysaccharide	C-C chemokine receptor type 7	Homo sapiens (human)
regulation of type II interferon production	C-C chemokine receptor type 7	Homo sapiens (human)
regulation of interleukin-1 beta production	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of interleukin-12 production	C-C chemokine receptor type 7	Homo sapiens (human)
response to prostaglandin E	C-C chemokine receptor type 7	Homo sapiens (human)
chemokine (C-C motif) ligand 19 signaling pathway	C-C chemokine receptor type 7	Homo sapiens (human)
chemokine (C-C motif) ligand 21 signaling pathway	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	C-C chemokine receptor type 7	Homo sapiens (human)
negative thymic T cell selection	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of cell adhesion	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of protein kinase activity	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of JNK cascade	C-C chemokine receptor type 7	Homo sapiens (human)
homeostasis of number of cells	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of T cell receptor signaling pathway	C-C chemokine receptor type 7	Homo sapiens (human)
release of sequestered calcium ion into cytosol	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of filopodium assembly	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	C-C chemokine receptor type 7	Homo sapiens (human)
cellular response to cytokine stimulus	C-C chemokine receptor type 7	Homo sapiens (human)
response to nitric oxide	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of neutrophil chemotaxis	C-C chemokine receptor type 7	Homo sapiens (human)
lymphocyte migration into lymph node	C-C chemokine receptor type 7	Homo sapiens (human)
mature conventional dendritic cell differentiation	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of cell motility	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of dendritic cell chemotaxis	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of immunological synapse formation	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of T cell costimulation	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of glycoprotein biosynthetic process involved in immunological synapse formation	C-C chemokine receptor type 7	Homo sapiens (human)
regulation of dendritic cell dendrite assembly	C-C chemokine receptor type 7	Homo sapiens (human)
negative regulation of dendritic cell apoptotic process	C-C chemokine receptor type 7	Homo sapiens (human)
immune response	C-C chemokine receptor type 7	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	C-C chemokine receptor type 7	Homo sapiens (human)
calcium-mediated signaling	C-C chemokine receptor type 7	Homo sapiens (human)
cell chemotaxis	C-C chemokine receptor type 7	Homo sapiens (human)
cytokine-mediated signaling pathway	C-C chemokine receptor type 2	Homo sapiens (human)
blood vessel remodeling	C-C chemokine receptor type 2	Homo sapiens (human)
dendritic cell chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
monocyte chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of T cell cytokine production	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of T-helper 1 type immune response	C-C chemokine receptor type 2	Homo sapiens (human)
negative regulation of type 2 immune response	C-C chemokine receptor type 2	Homo sapiens (human)
intracellular calcium ion homeostasis	C-C chemokine receptor type 2	Homo sapiens (human)
chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
humoral immune response	C-C chemokine receptor type 2	Homo sapiens (human)
cellular defense response	C-C chemokine receptor type 2	Homo sapiens (human)
negative regulation of adenylate cyclase activity	C-C chemokine receptor type 2	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	C-C chemokine receptor type 2	Homo sapiens (human)
response to wounding	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of vascular endothelial growth factor production	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of T cell chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
negative regulation of angiogenesis	C-C chemokine receptor type 2	Homo sapiens (human)
sensory perception of pain	C-C chemokine receptor type 2	Homo sapiens (human)
cellular homeostasis	C-C chemokine receptor type 2	Homo sapiens (human)
hemopoiesis	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of type II interferon production	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of interleukin-2 production	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of tumor necrosis factor production	C-C chemokine receptor type 2	Homo sapiens (human)
monocyte extravasation	C-C chemokine receptor type 2	Homo sapiens (human)
T-helper 17 cell chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
negative regulation of eosinophil degranulation	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of T cell differentiation	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of alpha-beta T cell proliferation	C-C chemokine receptor type 2	Homo sapiens (human)
homeostasis of number of cells within a tissue	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of inflammatory response	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of inflammatory response	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of T cell activation	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	C-C chemokine receptor type 2	Homo sapiens (human)
leukocyte adhesion to vascular endothelial cell	C-C chemokine receptor type 2	Homo sapiens (human)
chemokine-mediated signaling pathway	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of monocyte chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of immune complex clearance by monocytes and macrophages	C-C chemokine receptor type 2	Homo sapiens (human)
inflammatory response to wounding	C-C chemokine receptor type 2	Homo sapiens (human)
neutrophil clearance	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of leukocyte tethering or rolling	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of NMDA glutamate receptor activity	C-C chemokine receptor type 2	Homo sapiens (human)
macrophage migration	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of macrophage migration	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of thymocyte migration	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of monocyte extravasation	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of CD8-positive, alpha-beta T cell extravasation	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of astrocyte chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of hematopoietic stem cell migration	C-C chemokine receptor type 2	Homo sapiens (human)
cell chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
calcium-mediated signaling	C-C chemokine receptor type 2	Homo sapiens (human)
inflammatory response	C-C chemokine receptor type 2	Homo sapiens (human)
immune response	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	C-C chemokine receptor type 2	Homo sapiens (human)
MAPK cascade	C-C chemokine receptor type 5	Homo sapiens (human)
dendritic cell chemotaxis	C-C chemokine receptor type 5	Homo sapiens (human)
calcium ion transport	C-C chemokine receptor type 5	Homo sapiens (human)
chemotaxis	C-C chemokine receptor type 5	Homo sapiens (human)
cellular defense response	C-C chemokine receptor type 5	Homo sapiens (human)
cell surface receptor signaling pathway	C-C chemokine receptor type 5	Homo sapiens (human)
G protein-coupled receptor signaling pathway	C-C chemokine receptor type 5	Homo sapiens (human)
cell-cell signaling	C-C chemokine receptor type 5	Homo sapiens (human)
release of sequestered calcium ion into cytosol by sarcoplasmic reticulum	C-C chemokine receptor type 5	Homo sapiens (human)
calcium-mediated signaling	C-C chemokine receptor type 5	Homo sapiens (human)
signaling	C-C chemokine receptor type 5	Homo sapiens (human)
symbiont entry into host cell	C-C chemokine receptor type 5	Homo sapiens (human)
chemokine-mediated signaling pathway	C-C chemokine receptor type 5	Homo sapiens (human)
response to cholesterol	C-C chemokine receptor type 5	Homo sapiens (human)
cellular response to lipopolysaccharide	C-C chemokine receptor type 5	Homo sapiens (human)
negative regulation of macrophage apoptotic process	C-C chemokine receptor type 5	Homo sapiens (human)
inflammatory response	C-C chemokine receptor type 5	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	C-C chemokine receptor type 5	Homo sapiens (human)
immune response	C-C chemokine receptor type 5	Homo sapiens (human)
cell chemotaxis	C-C chemokine receptor type 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor activity	C-C chemokine receptor type 7	Homo sapiens (human)
C-C chemokine receptor activity	C-C chemokine receptor type 7	Homo sapiens (human)
chemokine (C-C motif) ligand 19 binding	C-C chemokine receptor type 7	Homo sapiens (human)
chemokine (C-C motif) ligand 21 binding	C-C chemokine receptor type 7	Homo sapiens (human)
C-C motif chemokine 19 receptor activity	C-C chemokine receptor type 7	Homo sapiens (human)
C-C motif chemokine 21 receptor activity	C-C chemokine receptor type 7	Homo sapiens (human)
chemokine receptor activity	C-C chemokine receptor type 2	Homo sapiens (human)
protein binding	C-C chemokine receptor type 2	Homo sapiens (human)
CCR2 chemokine receptor binding	C-C chemokine receptor type 2	Homo sapiens (human)
chemokine (C-C motif) ligand 2 binding	C-C chemokine receptor type 2	Homo sapiens (human)
chemokine (C-C motif) ligand 12 binding	C-C chemokine receptor type 2	Homo sapiens (human)
chemokine (C-C motif) ligand 7 binding	C-C chemokine receptor type 2	Homo sapiens (human)
identical protein binding	C-C chemokine receptor type 2	Homo sapiens (human)
C-C chemokine binding	C-C chemokine receptor type 2	Homo sapiens (human)
C-C chemokine receptor activity	C-C chemokine receptor type 2	Homo sapiens (human)
virus receptor activity	C-C chemokine receptor type 5	Homo sapiens (human)
actin binding	C-C chemokine receptor type 5	Homo sapiens (human)
phosphatidylinositol phospholipase C activity	C-C chemokine receptor type 5	Homo sapiens (human)
chemokine receptor activity	C-C chemokine receptor type 5	Homo sapiens (human)
protein binding	C-C chemokine receptor type 5	Homo sapiens (human)
coreceptor activity	C-C chemokine receptor type 5	Homo sapiens (human)
C-C chemokine receptor activity	C-C chemokine receptor type 5	Homo sapiens (human)
C-C chemokine binding	C-C chemokine receptor type 5	Homo sapiens (human)
identical protein binding	C-C chemokine receptor type 5	Homo sapiens (human)
chemokine (C-C motif) ligand 5 binding	C-C chemokine receptor type 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
mitochondrion	C-C chemokine receptor type 7	Homo sapiens (human)
plasma membrane	C-C chemokine receptor type 7	Homo sapiens (human)
cell surface	C-C chemokine receptor type 7	Homo sapiens (human)
external side of plasma membrane	C-C chemokine receptor type 7	Homo sapiens (human)
fibrillar center	C-C chemokine receptor type 2	Homo sapiens (human)
cytoplasm	C-C chemokine receptor type 2	Homo sapiens (human)
cytosol	C-C chemokine receptor type 2	Homo sapiens (human)
plasma membrane	C-C chemokine receptor type 2	Homo sapiens (human)
membrane	C-C chemokine receptor type 2	Homo sapiens (human)
dendrite	C-C chemokine receptor type 2	Homo sapiens (human)
neuronal cell body	C-C chemokine receptor type 2	Homo sapiens (human)
perikaryon	C-C chemokine receptor type 2	Homo sapiens (human)
perinuclear region of cytoplasm	C-C chemokine receptor type 2	Homo sapiens (human)
cytoplasm	C-C chemokine receptor type 2	Homo sapiens (human)
external side of plasma membrane	C-C chemokine receptor type 2	Homo sapiens (human)
cell surface	C-C chemokine receptor type 5	Homo sapiens (human)
endosome	C-C chemokine receptor type 5	Homo sapiens (human)
plasma membrane	C-C chemokine receptor type 5	Homo sapiens (human)
external side of plasma membrane	C-C chemokine receptor type 5	Homo sapiens (human)
cell surface	C-C chemokine receptor type 5	Homo sapiens (human)
external side of plasma membrane	C-C chemokine receptor type 5	Homo sapiens (human)
cytoplasm	C-C chemokine receptor type 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID1546905	Inhibition of CCR2 (unknown origin)	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10	The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
AID1353545	Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	Recent updates for designing CCR5 antagonists as anti-retroviral agents.
AID708110	Antiviral activity against Human immunodeficiency virus 1 clinical isolate	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Chemokine receptor antagonists.
AID1546906	Inhibition of CCR7 (unknown origin)	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10	The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
AID707908	Lipophilicity, log P of the compound	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Chemokine receptor antagonists.
AID707915	Antagonist activity at CCR2 assessed as inhibition of CCL2 binding	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Chemokine receptor antagonists.
AID707914	Antagonist activity at CCR5 assessed as inhibition of CCL3 binding	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Chemokine receptor antagonists.
AID707899	Half life in human	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Chemokine receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	5 (9.62)	29.6817
2010's	29 (55.77)	24.3611
2020's	18 (34.62)	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	12 (23.08%)	5.53%
Reviews	13 (25.00%)	6.00%
Case Studies	1 (1.92%)	4.05%
Observational	0 (0.00%)	0.25%
Other	26 (50.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (18)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Open-label Rollover Study of Cenicriviroc for the Treatment of Liver Fibrosis in Adult Subjects With Nonalcoholic Steatohepatitis (NASH)[NCT03059446]	Phase 2	167 participants (Actual)	Interventional	2017-02-14	Terminated(stopped due to This study was terminated early due to lack of efficacy based on the results of Part I of the AURORA study.)
A Randomized, Double-blind, Multicenter Study to Assess the Safety, Tolerability, and Efficacy of a Combination Treatment of Tropifexor (LJN452) and Cenicriviroc (CVC) in Adult Patients With Nonalcoholic Steatohepatitis (NASH) and Liver Fibrosis[NCT03517540]	Phase 2	193 participants (Actual)	Interventional	2018-09-11	Completed
I-SPY COVID TRIAL: An Adaptive Platform Trial to Reduce Mortality and Ventilator Requirements for Critically Ill Patients[NCT04488081]	Phase 2	1,500 participants (Anticipated)	Interventional	2020-07-31	Recruiting
A Proof of Concept, Multiple Dose-Escalating Study to Evaluate the Antiviral Activity, Safety, and Pharmacokinetics of the CCR5 Antagonist TBR 652 in HIV 1-Infected, Antiretroviral Treatment-Experienced, CCR5 Antagonist-Naïve Patients[NCT01092104]	Phase 1/Phase 2	52 participants (Actual)	Interventional	2009-02-28	Completed
An Open Label, Phase 1 Study to Evaluate the Effect of Mile and Moderate Hepatic Impairment on the Multiple-Dose Pharmacokinetics of Cenicriviroc (CVC)[NCT02120547]	Phase 1	31 participants (Actual)	Interventional	2014-03-31	Completed
A Phase 1, Single and Multiple-Dose, Open-Label Study in Healthy Subjects to Assess the Effect of the Acid Reducing Agents, Omeprazole (OME) and Famotidine (FAM), on the Pharmacokinetics (PK) of Cenicriviroc Mesylate (CVC)[NCT02684799]	Phase 1	48 participants (Actual)	Interventional	2016-01-31	Completed
A Phase 2b Randomized, Double-Blind, Double-Dummy Trial of 100 or 200 mg Once-Daily Doses of Cenicriviroc (CVC, TBR 652) or Once-Daily EFV, Each With Open-Label FTC/TDF, in HIV 1-Infected, Antiretroviral Treatment-Naïve, Adult Patients With Only CCR5-Trop[NCT01338883]	Phase 2	143 participants (Actual)	Interventional	2011-06-30	Completed
A Multicenter, Prospective, Double-Blind, Placebo-Controlled Study to Evaluate the Effects of Cenicriviroc Mesylate on Arterial Inflammation in People Living With HIV[NCT04334915]	Phase 2	0 participants (Actual)	Interventional	2022-11-22	Withdrawn(stopped due to Industry supporter no longer supporting the study. Protocol A5415's study will run instead.)
Charité Trial of Cenicriviroc (CVC) Treatment for COVID-19 Patients[NCT04500418]	Phase 2	45 participants (Actual)	Interventional	2020-08-25	Terminated(stopped due to Despite multiple efforts, no further patient could be enrolled since 03/05/2021. A continuation of the study is therefore no longer justified)
Randomized Master Protocol for Immune Modulators for Treating COVID-19[NCT04593940]	Phase 3	1,971 participants (Actual)	Interventional	2020-10-15	Completed
A Phase 1, Multiple-Dose, Open-Label, Randomized, Crossover Study in Healthy Subjects to Assess the Effect of Pioglitazone (PGZ) on the Pharmacokinetics (PK) of Cenicriviroc Mesylate (CVC) and the Effect of CVC on the PK of PGZ[NCT02342067]	Phase 1	20 participants (Actual)	Interventional	2014-12-31	Completed
A Phase I, Multiple-Dose, Open-Label, Crossover Study in Healthy Subjects to Assess the Effect of Dolutegravir (DTG) on the Pharmacokinetics (PK) of Cenicriviroc (CVC) and the Effect of CVC on the PK of DTG and on a Single Dose of Midazolam[NCT01827540]	Phase 1	20 participants (Actual)	Interventional	2013-03-31	Completed
PERSEUS: A Phase 2 Proof of Concept Study Investigating the Preliminary Efficacy and Safety of Cenicriviroc in Adult Subjects With Primary Sclerosing Cholangitis (PSC)[NCT02653625]	Phase 2	24 participants (Actual)	Interventional	2016-03-14	Completed
H020: Single-Arm Open Label, Pilot Study of CCR5/CCR2 Inhibitor Cenicriviroc (CVC) for HIV Associated Neurocognitive Disorder (HAND)[NCT02128828]	Phase 2	20 participants (Actual)	Interventional	2014-04-30	Completed
AURORA: A Phase 3, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Cenicriviroc for the Treatment of Liver Fibrosis in Adult Subjects With Nonalcoholic Steatohepatitis[NCT03028740]	Phase 3	1,778 participants (Actual)	Interventional	2017-04-05	Terminated(stopped due to This study was terminated early due to lack of efficacy based on the results of the planned interim analysis of Part 1 data.)
An Open-Label Study to Evaluate the Effect of Severe Hepatic Impairment on the Pharmacokinetics of Cenicriviroc and Its Metabolites Following Single Dose Administration[NCT03376841]	Phase 1	16 participants (Actual)	Interventional	2017-06-06	Completed
ORION - Effect of CCR2 and CCR5 Antagonism by Cenicriviroc on Peripheral and Adipose Tissue Insulin Sensitivity in Adult Obese Subjects With Prediabetes or Type 2 Diabetes Mellitus and Suspected Non-Alcoholic Fatty Liver Disease (NAFLD)[NCT02330549]	Phase 2	45 participants (Actual)	Interventional	2015-07-17	Completed
CENTAUR: Efficacy and Safety Study of Cenicriviroc for the Treatment of Nonalcoholic Steatohepatitis (NASH) in Adult Subjects With Liver Fibrosis[NCT02217475]	Phase 2	289 participants (Actual)	Interventional	2014-09-18	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT02128828 (1) [back to overview]	Change From Baseline to Week 24 in Global Neuropsychological Performance
NCT02217475 (52) [back to overview]	Change From Baseline in Portal Inflammation Grade on Liver Biopsy at Year 2
NCT02217475 (52) [back to overview]	Change From Baseline in Portal Inflammation Grade on Liver Biopsy at Year 1
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Markers of Hepatic Fibrosis: Nonalcoholic Fatty Liver Disease (NAFLD) Fibrosis Score (NFS) at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Markers of Hepatic Fibrosis: NAFLD Fibrosis Score (NFS) at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Markers of Hepatic Fibrosis: Enhanced Liver Fibrosis Test (ELF) Score at Months 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Markers of Hepatic Fibrosis: Enhanced Liver Fibrosis Test (ELF) Score at Months 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Hyaluronic Acid at Months 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Hyaluronic Acid at Months 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Fibrosis-4 (FIB-4) at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Aspartate Aminotransferase to Platelet Count Ratio Index (APRI) at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Aspartate Aminotransferase to Platelet Count Ratio Index (APRI) at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Morphometric Quantitative Fat Content on Liver Biopsy at Year 2
NCT02217475 (52) [back to overview]	Change From Baseline in Morphometric Quantitative Fat Content on Liver Biopsy at Year 1
NCT02217475 (52) [back to overview]	Change From Baseline in Morphometric Quantitative Collagen on Liver Biopsy at Year 2
NCT02217475 (52) [back to overview]	Change From Baseline in Morphometric Quantitative Collagen on Liver Biopsy at Year 1
NCT02217475 (52) [back to overview]	Change From Baseline in Histologic Fibrosis Stage (NASH CRN System and Ishak Scale Score) at Year 2
NCT02217475 (52) [back to overview]	Change From Baseline in Histologic Fibrosis Stage (NASH CRN System and Ishak Scale Score) at Year 1
NCT02217475 (52) [back to overview]	Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Fibrosis-4 (FIB-4) at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Hip Circumference at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Hip Circumference at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Hepatic Tissue Fibrogenic Protein Alpha-Smooth Muscle Actin (α-SMA) at Year 2
NCT02217475 (52) [back to overview]	Change From Baseline in Hepatic Tissue Fibrogenic Protein Alpha-Smooth Muscle Actin (α-SMA) at Year 1
NCT02217475 (52) [back to overview]	Change From Baseline in Forearm Circumference at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Forearm Circumference at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Body Mass Index (BMI) at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Body Mass Index (BMI) at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Biomarkers of Hepatocyte Apoptosis: Caspase Cleaved (CK-18 [M-30]) Levels and Total M-65 (CK-18 [M-65]) Levels at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Biomarkers of Hepatocyte Apoptosis: Caspase Cleaved (CK-18 [M-30]) Levels and Total M-65 (CK-18 [M-65]) Levels at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Number of Participants With Resolution of NASH Using a Modified Definition Based on Categorical Features of NAS and no Concurrent Worsening of Fibrosis Stage at Year 2
NCT02217475 (52) [back to overview]	Number of Participants With Resolution of NASH Using a Modified Definition Based on Categorical Features of NAS and no Concurrent Worsening of Fibrosis Stage at Year 1
NCT02217475 (52) [back to overview]	Number of Participants With Improvement in Fibrosis by at Least 1 Stage (NASH CRN System) and no Worsening of Steatohepatitis at Year 2
NCT02217475 (52) [back to overview]	Number of Participants With Improvement in Fibrosis by at Least 1 Stage (NASH CRN System) and no Worsening of Steatohepatitis at Year 1
NCT02217475 (52) [back to overview]	Number of Participants With Hepatic Histological Improvement With a Minimum 2-Point Improvement in NAS With at Least a 1-point Improvement in More Than 1 Categorical Features of NAS and no Concurrent Worsening of Fibrosis Stage at Year 2
NCT02217475 (52) [back to overview]	Change From Baseline in the 3 Categorical Features of NAS (Steatosis, Lobular Inflammation, Hepatocellular Ballooning) at Year 1
NCT02217475 (52) [back to overview]	Number of Participants With Hepatic Histological Improvement With a Minimum 2-Point Improvement in NAS With at Least a 1-Point Improvement in More Than 1 Categorical Features of NAS and no Concurrent Worsening of Fibrosis Stage at Year 1
NCT02217475 (52) [back to overview]	Number of Participants With Hepatic Histological Improvement in NAS at Year 2
NCT02217475 (52) [back to overview]	Number of Participants With Complete Resolution of Steatohepatitis With no Concurrent Worsening of Fibrosis Stage at Year 2
NCT02217475 (52) [back to overview]	Number of Participants With Complete Resolution of Steatohepatitis With no Concurrent Worsening of Fibrosis Stage at Year 1
NCT02217475 (52) [back to overview]	Number of Participants With Complete Resolution of Steatohepatitis With no Concurrent Worsening of Fibrosis Stage and Improvement in Fibrosis by at Least 1 Stage (NASH CRN System) and no Worsening of Steatohepatitis at Year 2
NCT02217475 (52) [back to overview]	Number of Participants With Complete Resolution of Steatohepatitis With no Concurrent Worsening of Fibrosis Stage and Improvement in Fibrosis by at Least 1 Stage (NASH CRN System) and no Worsening of Steatohepatitis at Year 1
NCT02217475 (52) [back to overview]	Number of Participants With Clinically Significant Changes in Vital Signs
NCT02217475 (52) [back to overview]	Number of Participants With Clinically Abnormal in Electrocardiogram (ECG) Findings
NCT02217475 (52) [back to overview]	Number of Participant With Hepatic Histological Improvement in NAS by ≥ 2 Points With at Least 1-Point Reduction in Either Lobular Inflammation or Hepatocellular Ballooning and no Concurrent Worsening of Fibrosis at Year 1
NCT02217475 (52) [back to overview]	Change From Baseline in the 3 Categorical Features of NAS (Steatosis, Lobular Inflammation, Hepatocellular Ballooning) at Year 2
NCT02217475 (52) [back to overview]	Change From Baseline in Tricep Skinfold Thickness at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Tricep Skinfold Thickness at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Waist Circumference at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Waist Circumference at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Change From Baseline in Weight at Months 15, 18 and 24
NCT02217475 (52) [back to overview]	Change From Baseline in Weight at Months 3, 6 and 12
NCT02217475 (52) [back to overview]	Number of Participants With Clinical Laboratory Abnormalities
NCT02217475 (52) [back to overview]	Number of Participants With Deaths, Treatment Emergent Adverse Events (TEAEs), Serious Adverse Events (SAEs), TEAEs Leading Study Drug to Discontinuation
NCT02330549 (55) [back to overview]	Change From Baseline in AUC (30-120 Min) for Serum FFA
NCT02330549 (55) [back to overview]	Change From Baseline in Biomarker of Inflammation: High Sensitivity C Reactive Protein (Hs-CRP)
NCT02330549 (55) [back to overview]	Change From Baseline in Biomarker of Inflammation: Interleukin 1 Beta (IL-1β)
NCT02330549 (55) [back to overview]	Change From Baseline in Biomarker of Inflammation: Interleukin 10 (IL-10)
NCT02330549 (55) [back to overview]	Change From Baseline in Biomarker of Inflammation: Interleukin 6 (IL-6)
NCT02330549 (55) [back to overview]	Change From Baseline in Biomarker of Inflammation: Interleukin 8 (IL-8)
NCT02330549 (55) [back to overview]	Change From Baseline in Biomarker of Inflammation: Tumor Necrosis Factor Alpha (TNF-α)
NCT02330549 (55) [back to overview]	Change From Baseline in Body Weight
NCT02330549 (55) [back to overview]	Change From Baseline in C-C Chemokine Receptor Type 2 (CCR2) and C-C Chemokine Receptor Type 5 (CCR5) in Subcutaneous Adipose Tissue
NCT02330549 (55) [back to overview]	Change From Baseline in Fasting Free Fatty Acids
NCT02330549 (55) [back to overview]	Change From Baseline in Fasting Glycosylated Hemoglobin A1c (HbA1c)
NCT02330549 (55) [back to overview]	Change From Baseline in Fasting Plasma Glucose (FPG)
NCT02330549 (55) [back to overview]	Change From Baseline in Fasting Plasma Insulin (FPI)
NCT02330549 (55) [back to overview]	Change From Baseline in Homeostasis Model Assessment of β-cell Function (HOMA-%B)
NCT02330549 (55) [back to overview]	Change From Baseline in Homeostasis Model of Insulin Resistance (HOMA-IR)
NCT02330549 (55) [back to overview]	Change From Baseline in Liver Transaminase: Alanine Aminotransferase (ALT)
NCT02330549 (55) [back to overview]	Change From Baseline in Liver Transaminase: Aspartate Aminotransferase (AST)
NCT02330549 (55) [back to overview]	Change From Baseline in Macrophage Infiltration in Subcutaneous Adipose Tissue
NCT02330549 (55) [back to overview]	Change From Baseline in Matsuda Index
NCT02330549 (55) [back to overview]	Change From Baseline in Non-invasive Imaging by Multiparametric Magnetic Resonance Imaging (MRI) for Liver Disease (LiverMultiScan™) Test: Corrected T1 (cT1)
NCT02330549 (55) [back to overview]	Change From Baseline in Non-invasive Imaging by Multiparametric Magnetic Resonance Imaging (MRI) for Liver Disease (LiverMultiScan™) Test: cT1 Mode Values Within the Liver
NCT02330549 (55) [back to overview]	Change From Baseline in Non-invasive Imaging by Multiparametric Magnetic Resonance Imaging (MRI) for Liver Disease (LiverMultiScan™) Test: Fat Fraction
NCT02330549 (55) [back to overview]	Change From Baseline in Non-invasive Imaging by Multiparametric Magnetic Resonance Imaging (MRI) for Liver Disease (LiverMultiScan™) Test: Iron Content
NCT02330549 (55) [back to overview]	Change From Baseline in Non-invasive Imaging by Multiparametric Magnetic Resonance Imaging (MRI) for Liver Disease (LiverMultiScan™) Test: Liver Inflammation and Fibrosis (LIF) Score
NCT02330549 (55) [back to overview]	Change From Baseline in Noninvasive Metabolic Biomarker: Cytokeratin-18 (CK-18) [M30 and M65]
NCT02330549 (55) [back to overview]	Change From Baseline in Noninvasive Metabolic Biomarker: Fibroblast Growth Factor-21 (FGF-21)
NCT02330549 (55) [back to overview]	Change From Baseline in Noninvasive Metabolic Biomarker: Hyaluronic Acid
NCT02330549 (55) [back to overview]	Change From Baseline in Noninvasive Metabolic Biomarker: Mac-2 Binding Protein (Mac-2BP)
NCT02330549 (55) [back to overview]	Change From Baseline in Noninvasive Metabolic Marker: Alpha-fetoprotein (AFP)
NCT02330549 (55) [back to overview]	Change From Baseline in Noninvasive Metabolic Serum Biomarker: Cluster of Differentiation (CD95)
NCT02330549 (55) [back to overview]	Change From Baseline in Peripheral Monocyte Subsets (CD14/CD16)
NCT02330549 (55) [back to overview]	Change From Baseline in Plasma Glucagon Concentration
NCT02330549 (55) [back to overview]	Change From Baseline in Quantitative Insulin Sensitivity Check Index (QUICKI)
NCT02330549 (55) [back to overview]	Change From Baseline in Serum Adiponectin Concentration
NCT02330549 (55) [back to overview]	Change From Baseline in Serum C-C Chemokine Receptor Type 2 (CCR2) Ligand: Monocyte Chemotactic Protein 1 (MCP-1)
NCT02330549 (55) [back to overview]	Change From Baseline in Serum C-C Chemokine Receptor Type 5 (CCR5) Ligand: RANTES
NCT02330549 (55) [back to overview]	Change From Baseline in Serum CCR5 Ligand: Macrophage Inflammatory Protein 1 Alpha (MIP-1α)
NCT02330549 (55) [back to overview]	Change From Baseline in Serum CCR5 Ligand: Macrophage Inflammatory Protein 1 Beta (MIP-1β)
NCT02330549 (55) [back to overview]	Change From Baseline in Serum Resistin Concentration
NCT02330549 (55) [back to overview]	Change From Baseline in the Nonalcoholic Fatty Liver Disease (NAFLD) Activity Score (NAS)
NCT02330549 (55) [back to overview]	Number of Participants by NASH Clinical Research Network (CRN) Staging Categories
NCT02330549 (55) [back to overview]	Number of Participants With Abnormal Physical Examination Findings
NCT02330549 (55) [back to overview]	Plasma Cenicriviroc Concentrations
NCT02330549 (55) [back to overview]	Plasma Glucose at 30, 60, 90 and 120 Minutes Following Glucose Load
NCT02330549 (55) [back to overview]	Plasma Insulin at 30, 60, 90 and 120 Minutes Following Glucose Load
NCT02330549 (55) [back to overview]	Serum FFA at 30, 60, 90 and 120 Minutes Following Glucose Load
NCT02330549 (55) [back to overview]	Number of Participants With at Least One Treatment-emergent Adverse Event (TEAE)
NCT02330549 (55) [back to overview]	Number of Participants With Clinically Relevant Changes From Baseline in Vital Signs
NCT02330549 (55) [back to overview]	Number of Participants With Clinically Significant Abnormal Electrocardiogram (ECG) Results
NCT02330549 (55) [back to overview]	Change From Baseline in Adipose Tissue Insulin Resistance (Adipo-IR ) Index
NCT02330549 (55) [back to overview]	Change From Baseline in Area Under the Concentration-time Curve From Time 0 to 120 Minutes [AUC (0-120 Min)] for Serum Glucose
NCT02330549 (55) [back to overview]	Change From Baseline in Area Under the Concentration-time Curve From Time 30 to 120 Minutes [AUC (30-120 Min)] for Serum Glucose
NCT02330549 (55) [back to overview]	Change From Baseline in AUC (0-120 Min) for Plasma Insulin
NCT02330549 (55) [back to overview]	Change From Baseline in AUC (0-120 Min) for Serum FFA
NCT02330549 (55) [back to overview]	Change From Baseline in AUC (30-120 Min) for Plasma Insulin
NCT02653625 (6) [back to overview]	Percentage of Participants With a Treatment-emergent Adverse Event (TEAE)
NCT02653625 (6) [back to overview]	Percentage of Participants Who Normalized ALP at Week 24
NCT02653625 (6) [back to overview]	Percentage of Participants Who Discontinued Due to a TEAE
NCT02653625 (6) [back to overview]	Percentage of Participants Who Achieved Serum ALP of Less Than 1.5 Times Upper Limit of Normal (ULN) in Serum ALP at Week 24
NCT02653625 (6) [back to overview]	Percentage of Participants Who Achieved a 50% Decrease in ALP at Week 24
NCT02653625 (6) [back to overview]	Percentage Change From Baseline Through Week 24 in Serum Alkaline Phosphatase (ALP)
NCT03028740 (9) [back to overview]	Time to First Occurrence of Adjudicated Events in the Full Study Cohort
NCT03028740 (9) [back to overview]	Percentage of Participants With Improvement in Fibrosis by at Least 2 Stages Regardless of Effect on Steatohepatitis on Liver Biopsy at Month 12 in the Full Study Cohort
NCT03028740 (9) [back to overview]	Percentage of Participants With Improvement in Fibrosis by at Least 2 Stages and No Worsening of Steatohepatitis on Liver Biopsy at Month 12 in the Full Study Cohort
NCT03028740 (9) [back to overview]	Percentage of Participants With Improvement in Fibrosis by at Least 1 Stage and No Worsening of Steatohepatitis on Liver Biopsy at Month 12 in the Full Study Cohort
NCT03028740 (9) [back to overview]	Part 1: Percentage of Participants With Improvement in Fibrosis by at Least 2 Stages Regardless of Effect on Steatohepatitis at Month 12
NCT03028740 (9) [back to overview]	Part 1: Percentage of Participants With Improvement in Fibrosis by at Least 2 Stages and No Worsening of Steatohepatitis on Liver Histology at Month 12
NCT03028740 (9) [back to overview]	Part 1: Percentage of Participants With Improvement in Fibrosis by at Least 1 Stage and No Worsening of Steatohepatitis on Liver Histology at Month 12
NCT03028740 (9) [back to overview]	Percentage of Participants With Improvement in Fibrosis by at Least 1 Stage Regardless of Effect on Steatohepatitis on Liver Biopsy at Month 12 in the Full Study Cohort
NCT03028740 (9) [back to overview]	Part 1: Percentage of Participants With Improvement in Fibrosis by at Least 1 Stage Regardless of Effect on Steatohepatitis at Month 12
NCT03059446 (1) [back to overview]	Number of Participants With Treatment-emergent Adverse Events (AE)
NCT03517540 (3) [back to overview]	Number of Participants With Adverse Events
NCT03517540 (3) [back to overview]	Proportion of Participants With Resolution of Steatohepatitis
NCT03517540 (3) [back to overview]	Proportion of Participants Who Have at Least a One Point Improvement in Fibrosis
NCT04593940 (24) [back to overview]	Number of Participants With Clinical Status for Day 28 Using an 8 Point Ordinal Scale
NCT04593940 (24) [back to overview]	Number of Participants With Clinical Status for Day 14 Using an 8 Point Ordinal Scale
NCT04593940 (24) [back to overview]	Number of Patients With SAEs Through Day 28
NCT04593940 (24) [back to overview]	Number of Patients With New Supplemental Oxygen Use
NCT04593940 (24) [back to overview]	Number of Patients With New Non-invasive Ventilation/High Flow Oxygen Use
NCT04593940 (24) [back to overview]	Number of Patients With New Mechanical Ventilation or ECMO Use
NCT04593940 (24) [back to overview]	Number of Patients With Grade 3 and 4 Adverse Events
NCT04593940 (24) [back to overview]	Number of Patients With Adverse Events Leading to Dose Modification
NCT04593940 (24) [back to overview]	Number of Participants Who Met a One Point Improvement in Two Categories From Day 0 (Baseline) to Day 28 Using an 8-point Ordinal Scale
NCT04593940 (24) [back to overview]	Number of Participants Who Had Recovered by Day 28
NCT04593940 (24) [back to overview]	Mortality Through 28 Days
NCT04593940 (24) [back to overview]	Mortality Through 14 Days
NCT04593940 (24) [back to overview]	Mean Change in the 8-point Ordinal Scale From Day 0 to Day 7
NCT04593940 (24) [back to overview]	Mean Change in the 8-point Ordinal Scale From Day 0 to Day 4
NCT04593940 (24) [back to overview]	Mean Change in the 8-point Ordinal Scale From Day 0 to Day 28
NCT04593940 (24) [back to overview]	Mean Change in the 8-point Ordinal Scale From Day 0 to Day 2
NCT04593940 (24) [back to overview]	Mean Change in the 8-point Ordinal Scale From Day 0 to Day 14
NCT04593940 (24) [back to overview]	Mean Change in the 8-point Ordinal Scale From Day 0 to Day 10
NCT04593940 (24) [back to overview]	Duration (Days) Alive and Out of the Hospital
NCT04593940 (24) [back to overview]	Mean Change in the 8-point Ordinal Scale From Day 0 to Day 21
NCT04593940 (24) [back to overview]	Duration (Days) Alive and Free of Supplemental Oxygen
NCT04593940 (24) [back to overview]	Duration (Days) Alive and Free of Non-invasive Ventilation/ High Flow Oxygen
NCT04593940 (24) [back to overview]	Duration (Days) Alive and Free of Invasive Mechanical Ventilation or ECMO
NCT04593940 (24) [back to overview]	Number of Participants Who Met a One Point Improvement in One Category From Day 0 (Baseline) to Day 28 Using an 8-point Ordinal Scale

Change From Baseline to Week 24 in Global Neuropsychological Performance

"Raw scores from individual performance on 14 validated neuropsychological tests meant to assess various cognitive domains were converted into standardized z-scores adjusted for age, sex, and education. Z-scores from all tests were aggregated and averaged to determine each subject's Global Neuropsychological Performance Score; NPZ-Global). Z-scores follow a normal distribution with scores < '0' identifying poorer cognition than 'average' and scores > 0 identifying better cognition than average with -1 and +1 represented 1 SD below or higher than average." (NCT02128828)
Timeframe: baseline, week 24

Intervention	units on a scale (Median)
Cenicriviroc	.24

Intervention	score on a scale (Mean)
	Baseline	Change from Baseline to Year 1
CVC 150 mg	1.6	0.2
Placebo	1.5	0.1

Intervention	ng/mL (Mean)
	Baseline (Month 3)	Change from Baseline to Month 3	Baseline (Month 6)	Change from Baseline to Month 6	Baseline (Month 12)	Change from Baseline to Month 12
CVC 150 mg	-1.012	0.087	-1.064	0.094	-1.040	0.139
Placebo	-1.227	0.029	-1.119	0.051	-1.132	0.121

Intervention	ng/mL (Mean)
	Baseline (Month 15)	Change from Baseline to Month 15	Baseline (Month 18)	Change from Baseline to Month 18	Baseline (Month 24)	Change from Baseline to Month 24
CVC 150 mg	-1.051	0.225	-1.057	0.196	-1.100	0.185
Placebo	-1.252	0.057	-1.284	0.046	-1.245	0.046

Intervention	percent fat area (Mean)
	Baseline	Change from Baseline to Year 2
CVC 150 mg	21.62	-2.96
Placebo	23.30	-5.06

Intervention	score on a scale (Mean)
	Baseline (NASH CRN Fibrosis Stage)	Change from Baseline (NASH CRN Fibrosis Stage)	Baseline (Ishak Fibrosis Stage)	Change from Baseline (Ishak Fibrosis Stage)
CVC 150 mg	2.1	0.0	2.2	0.0
Placebo	2.0	0.0	2.1	0.1

Intervention	U/L (Mean)
	CK-18(M30), Baseline (Month 15)	CK-18(M30), Change from Baseline to Month 15	CK-18(M30), Baseline (Month 18)	CK-18(M30), Change from Baseline to Month 18	CK-18(M30), Baseline (Month 24)	CK-18(M30), Change from Baseline to Month 24	CK-18(M65), Baseline (Month 15)	CK-18(M65), Change from Baseline to Month 15	CK-18(M65), Baseline (Month 18)	CK-18(M65), Change from Baseline to Month 18	CK-18(M65), Baseline (Month 24)	CK-18(M65), Change from Baseline to Month 24
CVC 150 mg	536.4	-13.3	540.9	57.3	541.8	39.7	687.4	88.6	694.8	181.5	693.9	124.9
Placebo	570.8	-39.6	578.8	23.8	575.4	-30.0	772.7	134.7	777.8	158.0	770.2	7.4

Intervention	score on a scale (Mean)
	Baseline (Steatosis)	Change from Baseline (Steatosis)	Baseline (Lobular Inflammation)	Change from Baseline (Lobular Inflammation)	Baseline (Hepatocellular Ballooning)	Change from Baseline (Hepatocellular Ballooning)
CVC 150 mg	1.3	-0.2	2.4	-0.1	1.5	-0.1
Placebo	1.4	-0.1	2.5	-0.1	1.5	-0.2

Intervention	Participants (Count of Participants)
	Fasting glucose (Grade 3)	Fasting glucose (Grade 4)	ALT (Grade 3)	ALT (Grade 4)	AST (Grade 3)	AST (Grade 4)	APT/PTT (Grade 3)	Triglycerides (Grade 3)	Triglycerides (Grade 4)	GGT (Grade 3)	GGT (Grade 4)	Creatine kinase (Grade 3)	Creatine kinase (Grade 4)	Uric acid (Grade 3)	Uric acid (Grade 4)	Amylase (Grade 3)	Amylase (Grade 4)	Lipase (Grade 3)	Lipase (Grade 4)	Phosphorus (Grade 3)	Phosphorus (Grade 4)	Absolute neutrophil (Grade 3)	Absolute neutrophil (Grade 4)
CVC 150 mg	10	0	4	0	1	0	1	6	2	8	1	1	3	4	5	4	2	3	3	2	0	3	1
CVC 150 mg (Year 1)	17	0	17	0	7	0	4	5	3	8	1	6	2	9	11	6	3	4	5	5	0	2	2
Placebo (Year 1)	13	0	17	0	10	0	2	7	3	7	1	7	2	8	6	1	0	2	0	2	0	3	1
Placebo Then CVC 150 mg	6	0	3	0	3	0	1	5	0	2	0	2	1	3	1	0	0	0	0	1	0	0	1
Placebo Then Placebo	5	0	2	0	1	0	2	2	1	2	0	4	0	2	6	1	0	1	1	1	0	1	1

Intervention	Participants (Count of Participants)
	Deaths	TEAEs	SAEs	TEAEs Leading Study Drug to Discontinuation
CVC 150 mg/CVC 150 mg	0	137	25	14
Placebo/CVC 150 mg	0	68	8	8
Placebo/Placebo	0	70	12	5

Intervention	min*mmol/L (Mean)
	Baseline	Change from Baseline to Week 12	Change from Baseline to Week 24
Cenicriviroc 150 mg	23.3	-5.0	-4.2
Placebo	25.6	-0.9	-1.5

Intervention	mg/L (Mean)
	Baseline	Change from Baseline to Week 2	Change from Baseline to Week 12	Change from Baseline to Week 24
Cenicriviroc 150 mg	6.39	-1.58	-0.50	-1.35
Placebo	5.39	0.12	2.33	0.14

Intervention	kg (Mean)
	Baseline	Change from Baseline to Week 2	Change from Baseline to Week 4	Change from Baseline to Week 8	Change from Baseline to Week 12	Change from Baseline to Week 16	Change from Baseline to Week 20	Change from Baseline to Week 24
Cenicriviroc 150 mg	94.92	-0.22	-0.52	0.21	0.53	0.87	0.17	0.03
Placebo	100.92	-1.10	-1.43	-1.56	-1.50	-1.73	-2.15	-2.44

Intervention	copies per sample (Median)
	CCR2, Baseline	CCR2, Change from Baseline to Week 24	CCR5, Baseline	CCR5, Change from Baseline to Week 24
Cenicriviroc 150 mg	13.0	2.6	12.7	3.6
Placebo	13.7	0.8	15.2	0.1

Intervention	cells/μL (Median)
	CD68+, Baseline	CD68+, Change from BL to Week 24	CD163+, Baseline	CD163+, Change from BL at Week 24	CCR2+, Baseline	CCR2+, Change from BL to Week 24	CCR5+, Baseline	CCR5+, Change from BL to Week 24	CD206+, Baseline	CD206+, Change from BL to Week 24
Cenicriviroc 150 mg	4.0	1.0	9.5	2.0	10.0	0.0	3.0	1.0	6.0	0.0
Placebo	3.0	1.0	10.5	1.0	10.5	2.0	3.0	0.0	7.0	-0.5

Intervention	cells/μL (Median)
	Total Monocytes, Baseline (BL)	Total Monocytes, Change from Baseline to Week 24	Classical Monocytes, Baseline	Classical Monocytes, Change from BL to Week 24	Intermediate Monocytes, Baseline	Intermediate Monocytes, Change from BL to Week 24	Non-Classical Monocytes, Baseline	Non-Classical Monocytes, Change from BL to Week 24
Cenicriviroc 150 mg	400	0	258	-43.6	16.8	-1.4	24.9	-7.1
Placebo	400	0	351	-31	22.4	3.8	30.9	-2.4

Intervention	Participants (Count of Participants)
	Baseline: Stage 0	Baseline: Stage 1	Baseline: Stage 1A	Baseline: Stage 1B	Baseline: Stage 1C	Baseline: Stage 2	Baseline: Stage 3	Baseline: Stage 4	Week 24: Stage 0	Week 24: Stage 1	Week 24: Stage 1A	Week 24: Stage 1B	Week 24: Stage 1C	Week 24: Stage 2	Week 24: Stage 3	Week 24 : Stage 4
Cenicriviroc 150 mg	2	2	1	0	0	0	1	0	2	3	0	0	0	0	1	0
Placebo	0	7	3	0	0	2	0	0	4	6	2	0	0	0	0	0

Intervention	ng/mL (Mean)
	Baseline: Pre-Dose	Week 2: Pre-Dose	Week 2: Post-Dose	Week 12: Pre-Dose	Week 12: Post-Dose	Week 24: Pre-Dose	Week 24: Post-Dose
Cenicriviroc 150 mg	0.0	168.7	170.7	383.3	320.4	230.7	127.4

Intervention	mg/dL (Mean)
	Week 12: Prior to Glucose Load	Week 12: 30 minutes	Week 12: 60 minutes	Week 12: 90 minutes	Week 12: 120 minutes	Week 24: Prior to Glucose Load	Week 24: 30 minutes	Week 24: 60 minutes	Week 24: 90 minutes	Week 24: 120 minutes
Cenicriviroc 150 mg	107.88	193.93	201.44	173.56	158.38	111.47	198.60	214.93	187.20	165.73
Placebo	119.39	205.90	232.74	227.00	201.04	114.88	198.65	232.09	220.61	191.26

Intervention	Participants (Count of Participants)
Arm A: Tropifexor (LJN452) - Dose 1	8
Arm B: Cenicriviroc (CVC)	8
Arm C: Tropifexor (LJN452) Dose 1 + CVC	5
Arm D: Tropifexor Dose 2 + CVC	9

Intervention	Participants (Count of Participants)
	1-Death	2-Hospitalized, on invasive mechanical ventilation or ECMO	3-Hospitalized, on non-invasive ventilation or high flow oxygen devices	4-Hospitalized, requiring supplemental oxygen	5-Hospitalized, not requiring supplemental oxygen - requiring ongoing medical in-patient care	6-Hospitalized, not requiring supplemental oxygen - no longer requires in-patient care	7-Not hospitalized, limitation on activities and/or requiring home oxygen	8-Not hospitalized
Standard of Care + Abatacept	56	27	5	10	8	1	149	231
Standard of Care + Abatacept Matching Placebo	77	26	8	12	5	2	156	207
Standard of Care + Cenicriviroc	49	25	7	4	2	0	109	142
Standard of Care + Cenicriviroc Matching Placebo	42	19	5	8	4	2	115	149
Standard of Care + Infliximab	53	28	6	11	3	2	135	258
Standard of Care + Infliximab Matching Placebo	75	27	7	10	6	2	156	217

cenicriviroc

Description

Cross-References

Synonyms (50)

Research Excerpts

Overview

Treatment

Toxicity

Pharmacokinetics

Bioavailability

Roles (5)

Drug Classes (6)

Protein Targets (4)

Inhibition Measurements

Biological Processes (105)

Molecular Functions (19)

Ceullar Components (13)

Bioassays (8)

Research

Studies (52)

Study Types

Clinical Trials (18)

Trial Overview

Trial Outcomes

Change From Baseline to Week 24 in Global Neuropsychological Performance

Change From Baseline in Portal Inflammation Grade on Liver Biopsy at Year 2

Change From Baseline in Portal Inflammation Grade on Liver Biopsy at Year 1

Change From Baseline in Non-invasive Markers of Hepatic Fibrosis: Nonalcoholic Fatty Liver Disease (NAFLD) Fibrosis Score (NFS) at Months 3, 6 and 12

Change From Baseline in Non-invasive Markers of Hepatic Fibrosis: NAFLD Fibrosis Score (NFS) at Months 15, 18 and 24

Change From Baseline in Non-invasive Markers of Hepatic Fibrosis: Enhanced Liver Fibrosis Test (ELF) Score at Months 6 and 12

Change From Baseline in Non-invasive Markers of Hepatic Fibrosis: Enhanced Liver Fibrosis Test (ELF) Score at Months 18 and 24

Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Hyaluronic Acid at Months 6 and 12

Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Hyaluronic Acid at Months 18 and 24

Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Fibrosis-4 (FIB-4) at Months 15, 18 and 24

Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Aspartate Aminotransferase to Platelet Count Ratio Index (APRI) at Months 3, 6 and 12

Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Aspartate Aminotransferase to Platelet Count Ratio Index (APRI) at Months 15, 18 and 24

Change From Baseline in Morphometric Quantitative Fat Content on Liver Biopsy at Year 2

Change From Baseline in Morphometric Quantitative Fat Content on Liver Biopsy at Year 1

Change From Baseline in Morphometric Quantitative Collagen on Liver Biopsy at Year 2

Change From Baseline in Morphometric Quantitative Collagen on Liver Biopsy at Year 1

Change From Baseline in Histologic Fibrosis Stage (NASH CRN System and Ishak Scale Score) at Year 2

Change From Baseline in Histologic Fibrosis Stage (NASH CRN System and Ishak Scale Score) at Year 1

Change From Baseline in Non-invasive Marker of Hepatic Fibrosis: Fibrosis-4 (FIB-4) at Months 3, 6 and 12

Change From Baseline in Hip Circumference at Months 3, 6 and 12

Change From Baseline in Hip Circumference at Months 15, 18 and 24

Change From Baseline in Hepatic Tissue Fibrogenic Protein Alpha-Smooth Muscle Actin (α-SMA) at Year 2

Change From Baseline in Hepatic Tissue Fibrogenic Protein Alpha-Smooth Muscle Actin (α-SMA) at Year 1

Change From Baseline in Forearm Circumference at Months 3, 6 and 12

Change From Baseline in Forearm Circumference at Months 15, 18 and 24

Change From Baseline in Body Mass Index (BMI) at Months 3, 6 and 12

Change From Baseline in Body Mass Index (BMI) at Months 15, 18 and 24

Change From Baseline in Biomarkers of Hepatocyte Apoptosis: Caspase Cleaved (CK-18 [M-30]) Levels and Total M-65 (CK-18 [M-65]) Levels at Months 3, 6 and 12

Change From Baseline in Biomarkers of Hepatocyte Apoptosis: Caspase Cleaved (CK-18 [M-30]) Levels and Total M-65 (CK-18 [M-65]) Levels at Months 15, 18 and 24

Number of Participants With Resolution of NASH Using a Modified Definition Based on Categorical Features of NAS and no Concurrent Worsening of Fibrosis Stage at Year 2

Number of Participants With Resolution of NASH Using a Modified Definition Based on Categorical Features of NAS and no Concurrent Worsening of Fibrosis Stage at Year 1

Number of Participants With Improvement in Fibrosis by at Least 1 Stage (NASH CRN System) and no Worsening of Steatohepatitis at Year 2

Number of Participants With Improvement in Fibrosis by at Least 1 Stage (NASH CRN System) and no Worsening of Steatohepatitis at Year 1

Number of Participants With Hepatic Histological Improvement With a Minimum 2-Point Improvement in NAS With at Least a 1-point Improvement in More Than 1 Categorical Features of NAS and no Concurrent Worsening of Fibrosis Stage at Year 2

Change From Baseline in the 3 Categorical Features of NAS (Steatosis, Lobular Inflammation, Hepatocellular Ballooning) at Year 1

Number of Participants With Hepatic Histological Improvement With a Minimum 2-Point Improvement in NAS With at Least a 1-Point Improvement in More Than 1 Categorical Features of NAS and no Concurrent Worsening of Fibrosis Stage at Year 1

Number of Participants With Hepatic Histological Improvement in NAS at Year 2

Number of Participants With Complete Resolution of Steatohepatitis With no Concurrent Worsening of Fibrosis Stage at Year 2

Number of Participants With Complete Resolution of Steatohepatitis With no Concurrent Worsening of Fibrosis Stage at Year 1

Number of Participants With Complete Resolution of Steatohepatitis With no Concurrent Worsening of Fibrosis Stage and Improvement in Fibrosis by at Least 1 Stage (NASH CRN System) and no Worsening of Steatohepatitis at Year 2

Number of Participants With Complete Resolution of Steatohepatitis With no Concurrent Worsening of Fibrosis Stage and Improvement in Fibrosis by at Least 1 Stage (NASH CRN System) and no Worsening of Steatohepatitis at Year 1

Number of Participants With Clinically Significant Changes in Vital Signs

Number of Participants With Clinically Abnormal in Electrocardiogram (ECG) Findings

Number of Participant With Hepatic Histological Improvement in NAS by ≥ 2 Points With at Least 1-Point Reduction in Either Lobular Inflammation or Hepatocellular Ballooning and no Concurrent Worsening of Fibrosis at Year 1

Change From Baseline in the 3 Categorical Features of NAS (Steatosis, Lobular Inflammation, Hepatocellular Ballooning) at Year 2

Change From Baseline in Tricep Skinfold Thickness at Months 15, 18 and 24

Change From Baseline in Tricep Skinfold Thickness at Months 3, 6 and 12

Change From Baseline in Waist Circumference at Months 15, 18 and 24

Change From Baseline in Waist Circumference at Months 3, 6 and 12

Change From Baseline in Weight at Months 15, 18 and 24

Change From Baseline in Weight at Months 3, 6 and 12

Number of Participants With Clinical Laboratory Abnormalities

Number of Participants With Deaths, Treatment Emergent Adverse Events (TEAEs), Serious Adverse Events (SAEs), TEAEs Leading Study Drug to Discontinuation

Change From Baseline in AUC (30-120 Min) for Serum FFA

Change From Baseline in Biomarker of Inflammation: High Sensitivity C Reactive Protein (Hs-CRP)

Change From Baseline in Biomarker of Inflammation: Interleukin 1 Beta (IL-1β)

Intervention	days (Mean)
Standard of Care + Infliximab	14.7
Standard of Care + Infliximab Matching Placebo	13.8
Standard of Care + Abatacept	14.1
Standard of Care + Abatacept Matching Placebo	13.7
Standard of Care + Cenicriviroc	14.2
Standard of Care + Cenicriviroc Matching Placebo	14.3

Intervention	days (Mean)
Standard of Care + Infliximab	16.3
Standard of Care + Infliximab Matching Placebo	15.2
Standard of Care + Abatacept	15.7
Standard of Care + Abatacept Matching Placebo	15.0
Standard of Care + Cenicriviroc	15.3
Standard of Care + Cenicriviroc Matching Placebo	15.8

Intervention	days (Mean)
Standard of Care + Infliximab	20.7
Standard of Care + Infliximab Matching Placebo	19.5
Standard of Care + Abatacept	20.3
Standard of Care + Abatacept Matching Placebo	19.3
Standard of Care + Cenicriviroc	19.4
Standard of Care + Cenicriviroc Matching Placebo	20.1

Intervention	days (Mean)
Standard of Care + Infliximab	23.4
Standard of Care + Infliximab Matching Placebo	22.6
Standard of Care + Abatacept	23.4
Standard of Care + Abatacept Matching Placebo	22.6
Standard of Care + Cenicriviroc	22.4
Standard of Care + Cenicriviroc Matching Placebo	23.2

Substance	Relationship Strength	Studies	Trials	Classes	Roles
uracil 2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder	4.03	3	0	pyrimidine nucleobase; pyrimidone	allergen; Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; prodrug; Saccharomyces cerevisiae metabolite
fenofibrate Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE	3.35	1	0	aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes	antilipemic drug; environmental contaminant; geroprotector; xenobiotic
avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.	2.07	1	0	azaspiro compound; biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.	3.31	1	0	guanidines	environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic
pioglitazone Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.	3.35	1	0	aromatic ether; pyridines; thiazolidinediones	antidepressant; cardioprotective agent; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; geroprotector; hypoglycemic agent; insulin-sensitizing drug; PPARgamma agonist; xenobiotic
carbon tetrachloride Carbon Tetrachloride: A solvent for oils, fats, lacquers, varnishes, rubber waxes, and resins, and a starting material in the manufacturing of organic compounds. Poisoning by inhalation, ingestion or skin absorption is possible and may be fatal. (Merck Index, 11th ed). tetrachloromethane : A chlorocarbon that is methane in which all the hydrogens have been replaced by chloro groups.	2.15	1	0	chlorocarbon; chloromethanes	hepatotoxic agent; refrigerant
cysteamine Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.. cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2.	3.27	1	0	amine; thiol	geroprotector; human metabolite; mouse metabolite; radiation protective agent
isoxazoles Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.	4.55	1	1	isoxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
oxazoles Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.	3.41	1	0	1,3-oxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
chenodeoxycholic acid Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3.	5.88	6	0	bile acid; C24-steroid; dihydroxy-5beta-cholanic acid	human metabolite; mouse metabolite
eosine yellowish-(ys) Eosine Yellowish-(YS): A versatile red dye used in cosmetics, pharmaceuticals, textiles, etc., and as tissue stain, vital stain, and counterstain with HEMATOXYLIN. It is also used in special culture media.. eosin YS dye : An organic sodium salt that is 2',4',5',7'-tetrabromofluorescein in which the carboxy group and the phenolic hydroxy group have been deprotonated and the resulting charge is neutralised by two sodium ions.	2.41	1	0	organic sodium salt; organobromine compound	fluorochrome; histological dye
ursodeoxycholic acid Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.	3.69	2	0	bile acid; C24-steroid; dihydroxy-5beta-cholanic acid	human metabolite; mouse metabolite
zidovudine Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.	3.13	1	0	azide; pyrimidine 2',3'-dideoxyribonucleoside	antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor
bezafibrate [no description available]	2.17	1	0	aromatic ether; monocarboxylic acid amide; monocarboxylic acid; monochlorobenzenes	antilipemic drug; environmental contaminant; geroprotector; xenobiotic
efavirenz efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.	10.87	2	1	acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound	antiviral drug; HIV-1 reverse transcriptase inhibitor
glucose, (beta-d)-isomer beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.	3.41	1	0	D-glucopyranose	epitope; mouse metabolite
fenofibric acid fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.	3.35	1	0	aromatic ketone; chlorobenzophenone; monocarboxylic acid	drug metabolite; marine xenobiotic metabolite
plerixafor plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma.	2.07	1	0	azacycloalkane; azamacrocycle; benzenes; crown amine; secondary amino compound; tertiary amino compound	anti-HIV agent; antineoplastic agent; C-X-C chemokine receptor type 4 antagonist; immunological adjuvant
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	3.62	2	0	1,2,3-triazole
rosiglitazone [no description available]	3.35	1	0	aminopyridine; thiazolidinediones	EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug
10-methyl spiro(4.5)dec-6-en-6-carboxylic acid 10-methyl spiro(4.5)dec-6-en-6-carboxylic acid: structure given in first source	3.7	1	0
tak 779 [no description available]	3.63	2	0
24-norursodeoxycholic acid 24-norursodeoxycholic acid: structure given in first source	3.31	1	0
tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.	2.58	2	0	retinoic acid; vitamin A	anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule
obeticholic acid obeticholic acid: A farnesoid X receptor agonist and anticholestatic agent that is used in the treatment of chronic liver diseases; structure in first source.. obeticholic acid : A dihydroxy-5beta-cholanic acid that is chenodeoxycholic acid carrying an additional ethyl substituent at the 6alpha-position. A semi-synthetic bile acid which acts as a farnesoid X receptor agonist and is used for treatment of primary biliary cholangitis.	5.88	6	0	3alpha-hydroxy steroid; 7alpha-hydroxy steroid; dihydroxy-5beta-cholanic acid	farnesoid X receptor agonist; hepatoprotective agent
bx 471 BX 471: a CC chemokine receptor-1 antagonist; structure in first source	2.07	1	0
buprenorphine Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.. buprenorphine : A morphinane alkaloid that is 7,8-dihydromorphine 6-O-methyl ether in which positions 6 and 14 are joined by a -CH2CH2- bridge, one of the hydrogens of the N-methyl group is substituted by cyclopropyl, and a hydrogen at position 7 is substituted by a 2-hydroxy-3,3-dimethylbutan-2-yl group. It is highly effective for the treatment of opioid use disorder and is also increasingly being used in the treatment of chronic pain.	2.25	1	0	morphinane alkaloid	delta-opioid receptor antagonist; kappa-opioid receptor antagonist; mu-opioid receptor agonist; opioid analgesic
aplaviroc aplaviroc: a spiro-diketo-piperazine; a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1; structure in first source	3.61	2	0
maraviroc [no description available]	10.27	8	0	tropane alkaloid
vicriviroc vicriviroc: structure in first source	3.61	2	0	(trifluoromethyl)benzenes
sb 225002 [no description available]	2.07	1	0	nitrophenol
pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.	2.17	1	0	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone	anti-inflammatory drug; bronchodilator agent; drug allergen
morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.	2.25	1	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
cp 481715 quinoxaline-2-carboxylic acid (4-carbamoyl-1-(3-fluorobenzyl)-2,7-dihydroxy-7-methyloctyl)amide: a CCR1 antagonist and NSAID; structure in first source	2.07	1	0
reparixin reparixin: inhibits CXCR1 to prevent polymorphonuclear cell recruitment	2.07	1	0	monoterpenoid
bms 193884 [no description available]	2.07	1	0
gft505 [no description available]	3.35	1	0
sch 527123 [no description available]	2.07	1	0
dapagliflozin [no description available]	3.35	1	0	aromatic ether; C-glycosyl compound; monochlorobenzenes	hypoglycemic agent; sodium-glucose transport protein subtype 2 inhibitor
gw 4064 [no description available]	3.35	1	0	stilbenoid
rs 504393 RS 504393: structure in first source	2.25	1	0	1,3-oxazoles
ccx282-b CCX282-B: antagonist of CCR9 chemokine receptor	2.07	1	0
ipragliflozin [no description available]	3.35	1	0	glycoside
sb 656933 [no description available]	2.07	1	0
mbx-8025 seladelpar: PPAR-delta agonist	3.35	1	0
empagliflozin [no description available]	4.29	2	0	aromatic ether; C-glycosyl compound; monochlorobenzenes; tetrahydrofuryl ether	hypoglycemic agent; sodium-glucose transport protein subtype 2 inhibitor
1,5-anhydro-1-(5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl)-1-thioglucitol [no description available]	3.35	1	0	diarylmethane
mgl-3196 resmetirom: a thyroid hormone receptor-beta agonist	4.03	3	0
liraglutide [no description available]	4.93	3	0	lipopeptide; polypeptide	glucagon-like peptide-1 receptor agonist; neuroprotective agent
glucagon-like peptide 1 Glucagon-Like Peptide 1: A peptide of 36 or 37 amino acids that is derived from PROGLUCAGON and mainly produced by the INTESTINAL L CELLS. GLP-1(1-37 or 1-36) is further N-terminally truncated resulting in GLP-1(7-37) or GLP-1-(7-36) which can be amidated. These GLP-1 peptides are known to enhance glucose-dependent INSULIN release, suppress GLUCAGON release and gastric emptying, lower BLOOD GLUCOSE, and reduce food intake.	3.31	1	0
incretins Incretins: Peptides which stimulate INSULIN release from the PANCREATIC BETA CELLS following oral nutrient ingestion, or postprandially.	3.27	1	0
aramchol [no description available]	2.25	1	0
raltegravir potassium Raltegravir Potassium: A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION.	2.21	1	0
canagliflozin canagliflozin hydrate : A hydrate that is the hemihydrate form of canagliflozin. Used for treatment of type II diabetes via inhibition of sodium-glucose transport protein subtype 2.	3.35	1	0	C-glycosyl compound; organofluorine compound; thiophenes	hypoglycemic agent; sodium-glucose transport protein subtype 2 inhibitor
amg 487 [no description available]	2.07	1	0
azd7687 AZD7687: structure in first source	3.35	1	0
sofosbuvir Sofosbuvir: A uridine monophosphate analog inhibitor of HEPATITIS C VIRUS (HCV) polymerase NS5B that is used as an ANTIVIRAL AGENT in the treatment of CHRONIC HEPATITIS C.. sofosbuvir : A nucleotide conjugate that is used in combination with ledipasvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection.	2.21	1	0	isopropyl ester; L-alanyl ester; nucleotide conjugate; organofluorine compound; phosphoramidate ester	antiviral drug; hepatitis C protease inhibitor; prodrug
raltegravir [no description available]	2.07	1	0	1,2,4-oxadiazole; dicarboxylic acid amide; hydroxypyrimidine; monofluorobenzenes; pyrimidone; secondary carboxamide	antiviral drug; HIV-1 integrase inhibitor
a 769662 [no description available]	3.35	1	0	biphenyls
4-(2-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl)methoxy)phenyl)cyclopropyl)benzoic acid 4-(2-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl)methoxy)phenyl)cyclopropyl)benzoic acid: a farnesoid X receptor agonist; structure in first source	3.35	1	0
icg 001 ICG 001: PRI-724 is an enantiomer of ICG-001; binds to cAMP response element-binding protein; structure in first source	3.31	1	0
pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.	3.31	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Autoimmune Disease [description not available]	0	2.07	1	0
Autoimmune Diseases Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.	0	2.07	1	0
HIV Coinfection [description not available]	0	9.46	13	3
HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	1	13.92	26	6
Cardiometabolic Syndrome A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY.	0	4.07	2	0
Fatty Liver, Nonalcoholic [description not available]	0	12.39	21	6
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	0	3.17	1	0
Metabolic Syndrome A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome include ABDOMINAL OBESITY; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state.	0	4.07	2	0
Non-alcoholic Fatty Liver Disease Fatty liver finding without excessive ALCOHOL CONSUMPTION.	1	17.01	42	12
Pericementitis [description not available]	0	2.41	1	0
Alveolar Bone Atrophy [description not available]	0	2.41	1	0
Periodontitis Inflammation and loss of connective tissues supporting or surrounding the teeth. This may involve any part of the PERIODONTIUM. Periodontitis is currently classified by disease progression (CHRONIC PERIODONTITIS; AGGRESSIVE PERIODONTITIS) instead of age of onset. (From 1999 International Workshop for a Classification of Periodontal Diseases and Conditions, American Academy of Periodontology)	0	7.41	1	0
Adverse Drug Event [description not available]	0	5.47	4	0
Cirrhosis, Liver [description not available]	0	11.84	16	6
Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.	0	11.84	16	6
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	5.47	4	0
2019 Novel Coronavirus Disease [description not available]	0	4.49	3	1
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	3.99	1	1
Cirrhosis [description not available]	0	4.94	2	1
Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.	0	9.94	2	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	4.66	5	0
Innate Inflammatory Response [description not available]	0	5.73	2	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	5.73	2	1
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted [description not available]	0	4.92	2	1
Hepatitis C INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown.	0	4.92	2	1
Insulin Sensitivity [description not available]	0	3.51	2	0
Insulin Resistance Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.	0	3.51	2	0
Disease Exacerbation [description not available]	0	7.7	6	2
Lesion of Sciatic Nerve [description not available]	0	2.66	2	0
Nerve Pain [description not available]	0	2.66	2	0
Neuralgia Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.	0	2.66	2	0
Infections, Coronavirus [description not available]	0	2.25	1	0
Pneumonia, Viral Inflammation of the lung parenchyma that is caused by a viral infection.	0	2.25	1	0
Coronavirus Infections Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).	0	2.25	1	0
Allodynia [description not available]	0	2.25	1	0
Disbacteriosis [description not available]	0	3.23	1	0
Acute Hepatic Failure [description not available]	0	2.15	1	0
Liver Failure, Acute A form of rapid-onset LIVER FAILURE, also known as fulminant hepatic failure, caused by severe liver injury or massive loss of HEPATOCYTES. It is characterized by sudden development of liver dysfunction and JAUNDICE. Acute liver failure may progress to exhibit cerebral dysfunction even HEPATIC COMA depending on the etiology that includes hepatic ISCHEMIA, drug toxicity, malignant infiltration, and viral hepatitis such as post-transfusion HEPATITIS B and HEPATITIS C.	0	2.15	1	0
Bile Duct Obstruction [description not available]	0	2.17	1	0
Liver Dysfunction [description not available]	0	4.46	4	1
Cholestasis Impairment of bile flow due to obstruction in small bile ducts (INTRAHEPATIC CHOLESTASIS) or obstruction in large bile ducts (EXTRAHEPATIC CHOLESTASIS).	0	2.17	1	0
Liver Diseases Pathological processes of the LIVER.	1	6.46	4	1
Becker Muscular Dystrophy [description not available]	0	2.17	1	0
Muscular Dystrophy, Duchenne An X-linked recessive muscle disease caused by an inability to synthesize DYSTROPHIN, which is involved with maintaining the integrity of the sarcolemma. Muscle fibers undergo a process that features degeneration and regeneration. Clinical manifestations include proximal weakness in the first few years of life, pseudohypertrophy, cardiomyopathy (see MYOCARDIAL DISEASES), and an increased incidence of impaired mentation. Becker muscular dystrophy is a closely related condition featuring a later onset of disease (usually adolescence) and a slowly progressive course. (Adams et al., Principles of Neurology, 6th ed, p1415)	0	2.17	1	0
Atherogenesis [description not available]	0	2.17	1	0
Atherosclerosis A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.	0	2.17	1	0
Co-infection [description not available]	0	4.51	1	1
Cognitive Decline [description not available]	0	2.21	1	0
Cognitive Dysfunction Diminished or impaired mental and/or intellectual function.	0	2.21	1	0
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	0	3.04	1	0
Acquired Immune Deficiency Syndrome [description not available]	0	2.94	1	0
Acquired Immunodeficiency Syndrome An acquired defect of cellular immunity associated with infection by the human immunodeficiency virus (HIV), a CD4-positive T-lymphocyte count under 200 cells/microliter or less than 14% of total lymphocytes, and increased susceptibility to opportunistic infections and malignant neoplasms. Clinical manifestations also include emaciation (wasting) and dementia. These elements reflect criteria for AIDS as defined by the CDC in 1993.	0	2.94	1	0