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NCI Drug Dictionary

82 results found for: U

UAE inhibitor TAK-243
A small molecule inhibitor of ubiquitin-activating enzyme (UAE), with potential antineoplastic activity. UAE inhibitor TAK-243 binds to and inhibits UAE, which prevents both protein ubiquitination and subsequent protein degradation by the proteasome. This results in an excess of proteins in the cells and may lead to endoplasmic reticulum (ER) stress-mediated apoptosis. This inhibits tumor cell proliferation and survival. UAE, also called ubiquitin E1 enzyme (UBA1; E1), is more active in cancer cells than in normal, healthy cells.
ubamatamab
A bispecific, human monoclonal antibody with potential antineoplastic activity. REGN4018 contains two antigen-recognition sites: one for human CD3, a T-cell surface antigen that is part of the T-cell receptor complex, and one for human mucin 16 (MUC16, cancer antigen 125; CA125; FLJ14303), a member of the mucin family of glycoproteins that is overexpressed by several epithelial cancers, including ovarian cancer. Upon administration, ubamatamab binds to both T cells and MUC16-expressing tumor cells, which cross-links the T cells to the tumor cells, and may result in a potent cytotoxic T-lymphocyte (CTL) response against the MUC16-expressing tumor cells.
ubavitinib tosylate
The tosylate salt form of NB003, an orally bioavailable inhibitor of specific mutated forms of platelet-derived growth factor receptor alpha (PDGFR alpha; PDGFRa) and mast/stem cell factor receptor c-Kit (SCFR; CD117), with potential antineoplastic activity. Upon oral administration, ubavitinib specifically targets, binds to and inhibits specific mutant forms of PDGFRa and c-Kit. This results in the inhibition of PDGFRa- and c-Kit-mediated signal transduction pathways and the inhibition of proliferation in tumor cells that express these PDGFRa and c-Kit mutants. PDGFRa and c-Kit, protein tyrosine kinases, are upregulated or mutated in various tumor cell types; they play key roles in the regulation of cellular proliferation and resistance to chemotherapy.
ubidecarenone nanodispersion BPM31510
A nanodispersion containing the benzoquinone ubidecarenone (coenzyme Q10), with potential protective, antioxidant and antineoplastic activities. Upon administration, ubidecarenone nanodispersion BPM31510 modulates tumor cell metabolism and causes an anti-Warburg effect by inducing a shift from lactate dependency towards mitochondrial oxidative phosphorylation, and induces tumor cell apoptosis. This inhibits tumor cell proliferation. BPM 31510 also induces the activation and maturation of T lymphocytes, and changes the surface expression of certain immune checkpoint modulators. In addition, as an antioxidant, ubidecarenone protects against cell damage, by preventing both the peroxidation of lipid membranes and the oxidation of LDL-cholesterol. Ubidecarenone is an essential coenzyme for mitochondrial enzyme complexes involved in oxidative phosphorylation and the production of adenosine triphosphate (ATP).
ublituximab
A chimeric recombinant IgG1 monoclonal antibody directed against human CD20 with potential antineoplastic activity. Ublituximab specifically binds to the B cell-specific cell surface antigen CD20, thereby potentially inducing a B cell-directed complement dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC) against CD20-expressing B cells, leading to B cell apoptosis. CD20 is a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B cell development and is often overexpressed in B-cell malignancies. Ublituximab has a specific glycosylation profile, with a low fucose content, that may enhance its ADCC response against malignant B cells.
udenafil
A benzenesulfonamide derivative with vasodilatory activity. Udenafil selectively inhibits phosphodiesterase type 5 (PDE5), thus inhibiting the degradation of cyclic guanosine monophosphate (cGMP) found in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis; inhibition of cGMP degradation results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, and, so, prolonged penile erection. This agent does not significantly inhibit the PDE11 isozyme; PDE11 inhibition may be associated with significant myalgia.
Udenyca
(Other name for: pegfilgrastim)
Ukoniq
(Other name for: umbralisib tosylate)
Ulcutin
(Other name for: proglumide)
ulimorelin hydrochloride
The hydrochloride salt form of ulimorelin, a macrocyclic ghrelin peptidomimetic, with potential gastrointestinal (GI) prokinetic activity. Upon intravenous administration, ulimorelin binds to the ghrelin receptor in the GI tract and may stimulate GI motility. Ghrelin is a natural ligand for growth hormone secretagogue receptors and is normally localized in the proximal GI tract. The ghrelin receptor signaling pathway mediates multiple GI functions, including motility and gastric emptying.
ulinastatin
A multivalent Kunitz-type serine protease inhibitor derived from human urine, with potential protective, anti-fibrinolytic and anticoagulant activities. Upon administration, ulinastatin (or urinary trypsinogen inhibitor) inhibits the activities of a variety of enzymes, including trypsin, chymotrypsin, thrombin, kallikrein, plasmin, elastase, cathepsin, lipase, hyaluronidase, factors IXa, Xa, XIa, and XlIa, and polymorphonuclear leukocyte elastase. In addition, ulinastatin inhibits the excessive release of proinflammatory mediators, such as tumor necrosis factor-alpha, interleukin-6 and -8, and chemokines. Altogether, this agent may improve the microcirculation, perfusion and function of tissues and may protect organ injury.
ulipristal acetate
An orally bioavailable, acetate ester of ulipristal, a selective progesterone receptor modulator with anti-progesterone activity. Ulipristal binds to the progesterone receptor (PR), thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system. As a result, this agent may suppress the growth of uterine leiomyomatosis. Furthermore, by inhibiting or delaying ovulation and effecting endometrial tissue, ulipristal can be used as an emergency contraception.
ulixertinib
An orally available inhibitor of extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity. Upon oral administration, ulixertinib inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.
ULK1/2 inhibitor DCC-3116
An orally bioavailable inhibitor of the serine/threonine-protein kinase ULK 1 and 2, with potential antineoplastic activity. Upon oral administration, ULK1/2 inhibitor DCC-3116 targets and binds to ULK1/2. This inhibits cancer autophagy, which mutant RAS cancer cells use for their survival, and results in tumor cell death. ULK1/2 mediates the autophagocytotic process and is often upregulated in cancers, especially in mutant RAS cancers. Autophagy plays a key role in a tumor cell proliferation and survival, and mediates tumor cell resistance.
ulocuplumab
An orally bioavailable monoclonal antibody against CXC chemokine receptor 4 (CXCR4) with potential antineoplastic activity. Ulocuplumab binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and subsequent receptor activation, which may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types.
Uloric
(Other name for: febuxostat)
Ultandren
(Other name for: fluoxymesterone)
Ultane
(Other name for: sevoflurane)
Ultiva
(Other name for: remifentanil hydrochloride)
Ultomiris
(Other name for: ravulizumab-cwvz)
ultra-micronized palmitoyl ethylamine (PEA) FSD-201
An orally bioavailable, ultra-micronized formulation of the fatty acid amide palmitoyl ethylamine (PEA), with potential anti-inflammatory activity. Upon oral administration, ultra-micronized PEA FSD-201 may inhibit both mast cell activation and migration, and the release of pro-inflammatory mediators from activated mast cells. This may reduce inflammation.
Ultradine
(Other name for: povidone-iodine solution)
Ultram
(Other name for: tramadol hydrochloride)
Ultravist
(Other name for: iopromide)
Ultresa
(Other name for: pancrelipase)
ulviprubart
A humanized, afucosylated monoclonal antibody directed against killer cell lectin-like receptor G1 (KLRG1), with potential immunomodulatory activity. Upon administration, anti-KLRG1 monoclonal antibody ABC008 targets and binds to KLRG1 expressed on highly differentiated effector CD8+ cytotoxic T cells, and selectively depletes these highly differentiated cytotoxic T cells while sparing other immune cells. This prevents the killing of cells by these highly differentiated cytotoxic T cells in certain autoimmune diseases, such as the destruction of muscle tissue in inclusion body myositis, and the destruction of neutrophils and red blood cell precursors in T-cell large granular lymphocytic leukemia (T-LGLL).
umbilical cord blood-derived CD16-expressing natural killer cells AB-101
A preparation of allogeneic, off-the-shelf natural killer (NK) cells, derived from umbilical cord blood (UCB) and ex vivo-expanded, that expresses a high-affinity variant of CD16, with potential immunostimulatory and antineoplastic activities. Upon administration, UCB-derived CD16-expressing NK cells AB-101 lyse tumor cells. NK cells AB-101 also secrete pro-inflammatory cytokines, which further stimulate an anti-tumor immune response. Upon coadministration with tumor-targeting monoclonal antibodies, the Fab moiety of the antibodies bind to the tumor-associated antigens (TAAs) expressed on tumor cells and the Fc moiety of the antibodies bind to CD16 expressed on NK cells AB-101. This leads to NK cell activation, cytokine secretion and antibody-dependent cellular cytotoxicity (ADCC). CD16, also known as Fc-gamma receptor III, is normally expressed on the surface of NK cells, neutrophils, monocytes and macrophages, and plays a key role in initiating ADCC. It is often downregulated in certain cancers, thereby inhibiting the anti-tumor immune response.
umbilical cord blood-derived CD4+/CD25+ T-regulatory cells CK0801
A preparation composed of allogeneic umbilical cord blood (UCB)-derived, ex vivo expanded and enhanced CD4+/CD25+ T-regulatory cells (Tregs) with potential immunomodulatory activity. Upon administration, the UCB-derived CD4+/CD25+ Tregs CK0801 may promote immunologic homeostasis and prevent autoimmunity by suppressing self-reactive T cells. This may induce tolerance to allogeneic organ transplants, prevent graft-versus-host disease (GvHD), and suppress autoimmune pathology.
umbilical cord blood-derived MAK immune cells
A preparation of mixed-activated killer (MAK) immune cells derived from human umbilical cord blood (UCB) cells, with potential cytotoxic activity. Hematopoietic stem cells (HSCs) are isolated followed by ex vivo differentiation and expansion. Upon administration, the UCB-derived MAK immune cells may lyse cancer cells.
umbilical cord blood-derived mesenchymal stem cells
Multipotent stem cells of mesenchymal origin isolated from umbilical cord blood. Umbilical cord blood-derived mesenchymal stem cells can differentiate into a variety of cell types including fibroblasts, osteoblasts, chondrocytes, myocytes, adipocytes, and endothelial cells.
umbilical cord blood-derived natural killer cells
A population of allogeneic, cytokine-differentiated, highly lytic natural killer (NK) cells derived from CD34+ cells isolated from human umbilical cord blood (UCB) with potential cytotoxic activity. CD34+ hematopoietic stem cells (HSC) are isolated from human UCB mononuclear cells, differentiated into mature, highly lytic, CD3- CD56+ NK cells, by a specific combination of cytokines that includes stem cell factor (SCF), fms-related tyrosine kinase 3 ligand (Flt3-L), interleukin-15 (IL-15) and insulin-like growth factor-1 (IGF-1), and expanded ex vivo. Upon administration, the UCB-derived NK cells may lyse cancer cells.
umbralisib tosylate
The tosylate form of umbralisib, an orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinases (PI3K) with potential antineoplastic activity. umbralisib inhibits PI3K and prevents the activation of the PI3K/AKT kinase signaling pathway. This decreases proliferation and induces cell death in susceptible tumor cells. Unlike other isoforms of PI3K, PI3K-delta is expressed primarily in tumor cells and cells of the hematopoietic lineage. The targeted inhibition of PI3K-delta allows for PI3K signaling in normal, non-neoplastic cells. PI3K, an enzyme often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival.
Unasyn
(Other name for: ampicillin sodium/sulbactam sodium)
Uncaria tomentosa extract
An extract of Uncaria tomentosa (U. tomentosa), also called Cat's claw, a native Amazonian plant belonging to the Rubiaceae species, with potential anti-inflammatory, immunomodulating, antioxidant and antineoplastic activities. Although the exact mechanism(s) by which U. tomentosa extract exerts its effect(s) has yet to be fully elucidated, this extract may inhibit the proliferation of certain types of cancer cells. This extract may modulate inflammatory and immune responses through the stimulation of T- and B-lymphocytes and certain cytokines, including interleukin (IL)-1, IL-6 and tumor necrosis factor-alpha (TNF-a). Components in U. tomentosa may both induce repair of chemically-induced DNA damage and scavenge free radicals, which may protect against reactive oxygen species (ROS)-mediated cellular damage. In addition, this extract stimulates myelopoiesis, which may prevent chemotherapy-induced neutropenia.
unesbulin
An orally active inhibitor of the polycomb ring finger oncogene BMI1 (B-cell-specific Moloney murine leukemia virus integration site 1), with potential antineoplastic activity. Upon oral administration, unesbulin targets BMI1 expressed by both tumor cells and cancer stem cells (CSCs), and induces hyper-phosphorylation of BMI1 leading to its degradation. This inhibits BMI1-mediated signal transduction pathways and results in a reduction of proliferation of BMI1-expressing tumor cells. BMI1, a key protein in the polycomb repressive complex 1 (PRC1), is overexpressed in certain tumor cell types, and plays a key role in CSC survival, proliferation and resistance to chemotherapeutics; its expression is associated with increased tumor aggressiveness and a poor prognosis.
uniformly-labeled [13C]fructose
A uniformly-labeled radioconjugate composed of the monosaccharide fructose in which all six carbons are labeled with the isotope carbon C 13 (13C), with potential imaging application. Upon administration of uniformly-labeled [13C]fructose, fructose is taken up and metabolized by tumors and the 13C-containing metabolites can be imaged by 13C nuclear magnetic resonance (NMR) spectroscopy. As certain tumor cells preferentially take up and metabolize fructose for fuel, this agent may help assess the extent of fructose metabolism in tumor cells.
Uniformly-labeled [13C]glucose
A non-radioactive, naturally occurring carbon 13 (13C) glucose isotopomer in which all six carbons are 13C, with potential imaging application. Upon administration of uniformly-labeled [U-13C] glucose, the glucose is taken up and metabolized by tumors and the 13C-containing metabolites can be imaged by 13C nuclear magnetic resonance (NMR) spectroscopy. Since tumor cells take up and metabolize glucose in higher amounts and through different pathways than normal cells, this agent may help assess the metabolic phenotype of the tumor.
uniformly-labeled [13C]glutamine
A uniformly-labeled radioconjugate composed of glutamine, a naturally occurring non-essential amino acid, in which all five carbons are labeled with the isotope 13C, with potential imaging application. Upon administration of uniformly-labeled [13C]glutamine, the glutamine is taken up and metabolized by tumors and the 13C-containing metabolites can be imaged by 13C nuclear magnetic resonance (NMR) spectroscopy. Since tumor cells take up and metabolize glutamine in higher amounts and through different pathways than normal cells, this agent may help assess the metabolic phenotype of the tumor.
uniformly-labeled [13C]lactate
A uniformly-labeled radioconjugate composed of lactate in which all three carbons are labeled with the isotope carbon C 13 (13C), with potential imaging application. Upon administration of uniformly-labeled [13C]lactate, lactate is taken up and metabolized by tumors, via the tricarboxylic acid (TCA) cycle, and the 13C-containing metabolites can be imaged by 13C nuclear magnetic resonance (NMR) spectroscopy. As certain tumor cells preferentially take up and metabolize lactate for fuel, this agent may help assess the extent of lactate metabolism in tumor cells.
Uniphyl
(Other name for: theophylline)
Unituxin
(Other name for: dinutuximab)
universal anti-CD7 CAR T cells RD13-01
A preparation of universal T lymphocytes that have been genetically engineered to express a chimeric antigen receptor (CAR) directed against the tumor-associated antigen (TAA) CD7, with potential immunostimulating and antineoplastic activities. Upon administration, universal anti-CD7 CAR T cells RD13-01 specifically recognize and bind to CD7-expressing tumor cells, resulting in specific T-cell-mediated tumor cell lysis. CD7 is a transmembrane glycoprotein expressed by T cells and natural killer (NK) cells and their precursors. It is expressed in the majority of lymphoblastic T-cell leukemias and lymphomas and in a subset of peripheral T-cell lymphomas.
universal donor expanded TGF-beta-imprinted NK cells
A preparation of ex vivo expanded, universal donor, transforming growth factor-beta (TGF-beta; TGF-b) imprinted natural killer (NK) cells, with potential cytolytic and antineoplastic activities. Upon administration, the universal donor expanded TGF-beta-imprinted NK cells may directly lyse cancer cells. These cells also secrete pro-inflammatory cytokines and further stimulate a systemic immune response against cancer cells. TGF-beta imprinting during NK cell activation and expansion decreases NK cell sensitivity to TGF-beta suppression and promotes NK cell cytokine hypersecretion, specifically of interferon-gamma (IFNg) and tumor necrosis factor-alpha (TNFa), and enhances NK cytotoxicity. TGF-beta is a potent immunosuppressive cytokine that inhibits the anti-tumor responses of NK cells and T cells.
Unloxcyt
(Other name for: cosibelimab-ipdl)
upacicalcet
An agonist of calcium-sensing receptors (CaSR), with potential use in the treatment of secondary hyperparathyroidism (SHPT). Upon administration, upacicalcet targets and binds to CaSRs expressed on the membranes of cells in the parathyroid glands, which suppresses osteoclast activity and reduces the excessive secretion of parathyroid hormone (PTH). This prevents the excessive PTH-mediated efflux of phosphorus and calcium from bone into the blood and normalizes serum calcium and phosphorus levels. Upacicalcet may decrease the risk of bone fracture, may lower depositions of phosphorus and calcium salts in non-bone tissues, may reduce bone and joint pain and may slow the progression of other diseases related to increased levels of PTH. CaSR controls calcium homeostasis and regulates the release of PTH.
upacicalcet sodium hydrate
The sodium hydrate form of upacicalcet, an agonist of calcium-sensing receptors (CaSR), with potential use in the treatment of secondary hyperparathyroidism (SHPT). Upon administration, upacicalcet targets and binds to CaSRs expressed on the membranes of cells in the parathyroid glands, which suppresses osteoclast activity and reduces the excessive secretion of parathyroid hormone (PTH). This prevents the excessive PTH-mediated efflux of phosphorus and calcium from bone into the blood and normalizes serum calcium and phosphorus levels. Upacicalcet may decrease the risk of bone fracture, may lower depositions of phosphorus and calcium salts in non-bone tissues, may reduce bone and joint pain and may slow the progression of other diseases related to increased levels of PTH. CaSR controls calcium homeostasis and regulates the release of PTH.
UPASITA
(Other name for: upacicalcet sodium hydrate)
upinitatug
A proprietary humanized monoclonal antibody against human sodium-dependent phosphate transport protein 2B (SLC34A2; NaPi2b), with potential antineoplastic activity. Upon administration of upinitatug, the antibody targets and binds to NaPi2b expressed on tumor cells. Although the tumor cell killing effects of upinitatug are not established, this binding may induce an antibody-dependent cellular cytotoxicity (ADCC)-mediated immune response against NaPi2b-expressing tumor cells, and/or may inhibit NaPi2b-mediated sodium and phosphate ion cotransport activity and ion-dependent tumor cell signaling. NaPi2b, a tumor-associated antigen (TAA), is overexpressed on a variety of tumor cells. It plays a key role in the transport of inorganic phosphate (Pi) and the maintenance of phosphate homeostasis.
upinitatug rilsodotin
A proprietary antibody-drug conjugate (ADC) composed of upinitatug , a proprietary, humanized monoclonal antibody against human sodium-dependent phosphate transport protein 2B (SLC34A2; NaPi2b), site-specifically linked, via a protease cleavable linker, to the proprietary cytotoxic aurastatin derivative auristatin F-HPA (AF-HPA; auristatin F-hydroxypropylamide), with potential antineoplastic activity. Upinitatug rilsodotin is produced via the proprietary dolaflexin ADC conjugation platform, which promotes the conjugation of between 10 and 15 AF-HPA payload molecules to each XMT-1535 antibody. Upon administration of upinitatug rilsodotin, the antibody moiety targets and binds to NaPi2b expressed on tumor cells. Upon binding, internalization by endosomes/lysosomes, and enzymatic cleavage, the AF-HPA binds to tubulin and inhibits microtubule polymerization, which results in G2/M phase arrest and apoptosis of NaPi2b-expressing tumor cells. NaPi2b, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer cells and plays a key role in the transport of inorganic phosphate (Pi) and the maintenance of phosphate homeostasis.
uproleselan
A synthetic, glycomimetic molecule and E-selectin (CD62E) antagonist, with potential anti-thrombotic, antineoplastic and chemopotentiating activities. Upon administration, uproleselan binds to E-selectin expressed on endothelial cells and prevents their interaction with selectin-E ligand-expressing cancer cells. This may prevent tumor cell activation, migration and metastasis. Uproleselan also interferes with the binding of selectin E-expressing vascular endothelial cells to selectin-E ligand-expressing monocytes and neutrophils, thereby disrupting their activation. Consequently, this inhibits both the activation of the coagulation cascade and thrombus formation. This agent also prevents both leukocyte activation and inflammation. E-selectin is a cell adhesion molecule involved in cell rolling, signaling and chemotaxis; it also plays a crucial role in inflammatory processes and cancer.
uracil
One of the 5 major bases (with adenine, guanine, cytosine, and thymine) which are a component of nucleic acids.
uracil ointment
A 0.1% topical formulation of uracil used to potentially lower the incidence of hand-foot syndrome (HFS) (or palmar-plantar erythrodysesthesia) during 5-fluorouracil (5-FU) or 5-FU prodrug capecitabine chemotherapy. Upon local administration of uracil ointment to the skin, uracil competes with capecitabine or 5-FU as substrates for the activating enzyme thymidine phosphorylase and the metabolizing enzyme dihydropyrimidine dehydrogenase. This may prevent the production of 5-FU as well as the breakdown of 5-FU into the toxic metabolites locally. As the 5-FU metabolites are responsible for the presentation of HFS, inhibiting their formation may prevent this adverse effect. By applying a high concentration of uracil locally, the skin toxicities of 5-FU may be countered while preserving the systemic anti-cancer activity of the 5FU.
urelumab
A humanized agonistic monoclonal antibody targeting the CD137 receptor with potential immunostimulatory and antineoplastic activities. Urelumab specifically binds to and activates CD137-expressing immune cells, stimulating an immune response, in particular a cytotoxic T cell response, against tumor cells. CD137 is a member of the tumor necrosis factor (TNF)/nerve growth factor (NGF) family of receptors and is expressed by activated T- and B-lymphocytes and monocytes; its ligand has been found to play an important role in the regulation of immune responses.
uridine
A nucleoside consisting of uracil and D-ribose and a component of RNA. Uridine has been studied as a rescue agent to reduce the toxicities associated with 5-fluorouracil (5-FU), thereby allowing the administration of higher doses of 5-FU in chemotherapy regimens.
uridine phosphorylase inhibitor TK-112690
A 2,2'-anhydropyrimidine derivative and human uridine phosphorylase (UPase) inhibitor that can be used to suppress mucositis induced by certain chemotherapeutics. Upon administration of UPase inhibitor TK-112690 prior to the administration of certain chemotherapeutic agents, such as methotrexate (MTX), this agent targets, binds to and blocks the activity of UPase, thereby preventing the metabolic breakdown of uridine into uracil. This increases the uridine levels in plasma and may prevent mucositis. By rescuing normal tissue, TK-112690 may enhance the therapeutic index of the chemotherapeutic agent. UPase plays a key role in in pyrimidine metabolism, and catabolizes uridine into uracil and ribose-1-phosphate.
uridine triacetate
An orally bioavailable, lipophilic, triacetate prodrug form of the pyrimidine nucleoside, uridine, that can be used for uridine replacement or as an antidote for 5-fluorouracil (5-FU)-induced toxicity. Upon administration, uridine triacetate is deacetylated by esterases to produce uridine and acetate. In turn, uridine is converted to uridine triphosphate (UTP), which competes with fluorouridine triphosphate (FUTP), one of the toxic metabolites of 5-FU, for incorporation into RNA of normal cells. This prevents disruption of RNA synthesis in normal cells and limits toxicity resulting from overdose of 5-FU and 5-FU prodrugs. The FUTP-mediated damage to RNA is the main cause of 5-FU toxicities.
URLC10 peptide/Montanide ISA51 vaccine
A cancer vaccine containing URLC10 (up-regulated lung cancer 10) epitopes with potential immunostimulatory and antineoplastic activities. Upon administration, URL peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URLC10-expressing tumor cells. Up-regulated in lung and esophageal cancers, the function of URLC10 is unknown.
URLC10-CDCA1-KOC1 multipeptide vaccine
A cancer vaccine containing multiple peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from, URLC10 (up-regulated lung cancer 10), CDCA1 (cell division cycle-associated protein 1), KOC1 (IGF II mRNA Binding Protein 3). Upon administration, URLC10-CDCA1-KOC1 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing URLC10, CDCA1, KCO1 peptides, resulting in cell lysis and decreased tumor growth.
URLC10-TTK-KOC1-VEGFR1-VEGFR2 multipeptide vaccine
A cancer vaccine containing five peptide epitopes with potential immunostimulatory and antitumor activity. Peptide epitopes in this vaccine are derived from: URLC10 (up-regulated lung cancer 10), TTK (TTK protein kinase), KOC1 (IGF II mRNA Binding Protein 3) and VEGFRs (vascular endothelial growth factor receptors) 1 and 2. Upon administration, URLC10-TTK-KOC1-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing URLC10, TTK, KCO1, VEGFR 1 and 2 peptides, resulting in cell lysis and decreased tumor growth.
urokinase-derived peptide A6
An octapeptide (amino acids 136-143) derived from the proteolytic enzyme urokinase plasminogen activator (uPA), with potential antineoplastic activity. A6 is derived from the nonreceptor-binding domain and connecting region of urokinase. Administration of A6 inhibits the interaction of uPA with its receptor uPAR, and may inhibit endothelial cell motility and tumor cell invasion. uPA and uPAR promote extracellular matrix degradation and growth factor activation and correlate positively with angiogenesis, cancer cell invasion and metastasis.
Urolene Blue
(Other name for: methylene blue)
urolithin A supplement
A dietary supplement composed of urolithin A (Uro-A) that may be used to modulate mitochondrial activity, and with potential antioxidant and anti-inflammatory activities. Upon oral administration, urolithin A supplement activates mitophagy, which may improve mitochondrial and cellular health. Urolithin A, one of the natural polyphenolic metabolites of ellagic acid and ellagitannins produced by the gut microbiota, also acts as a direct free radical scavenger, which may protect against inflammation- and reactive oxygen species (ROS)-induced cellular damage.
Uroplus
(Other name for: Trimethoprim-Sulfamethoxazole)
Uroxatral
(Other name for: alfuzosin hydrochloride)
URSO
(Other name for: ursodiol)
ursodiol
A synthetically-derived form of ursodiol, a bile acid produced by the liver and secreted and stored in the gallbladder. Also produced by the Chinese black bear liver, ursodiol has been used in the treatment of liver disease for centuries. This agent dissolves or prevents cholesterol gallstones by blocking hepatic cholesterol production and decreasing bile cholesterol. Ursodiol also reduces the absorption of cholesterol from the intestinal tract.
ursolic acid
A pentacyclic triterpenoid found in various fruits, vegetables and medicinal herbs, with a variety of potential pharmacologic activities including anti-inflammatory, antioxidative, antiviral, serum lipid-lowering, and antineoplastic activities. Upon administration, ursolic acid may promote apoptosis and inhibit cancer cell proliferation through multiple mechanisms. This may include the regulation of mitochondrial function through various pathways including the ROCK/PTEN and p53 pathways, the suppression of the nuclear factor-kappa B (NF-kB) pathways, and the increase in caspase-3, caspase-8 and caspase-9 activities.
Urtica dioica extract
An extract of Urtica dioica (stinging nettle; common nettle), a herbaceous perennial flowering plant in the family Urticaceae, with potential antioxidant, anti-inflammatory, antibacterial, anti-anemia and anti-hypertensive activities, and may help control fatigue. Urtica dioica extract contains a wide variety of phytochemicals, including, but not limited to, vitamins, minerals, fatty acids, essential amino acids, polyphenols and carotenoids. Upon oral administration, the active ingredients in Urtica dioica may exert a wide variety of effects.
USP1 inhibitor HSK39775
An orally bioavailable small molecule inhibitor of the human deubiquitinating enzyme ubiquitin specific protease 1 (USP1; ubiquitin carboxyl-terminal hydrolase 1), with potential antineoplastic activity. Upon oral administration, USP1 inhibitor HSK39775 specifically targets, binds to and inhibits the activity of USP1, thereby blocking complex formation of USP1 with USP1-associated factor 1 (UAF1), and inhibits USP1-mediated deubiquitinating activity. This may result in replication fork degradation, accumulation of mono-ubiquinated substrates, inhibition of DNA damage repair, induction of cell cycle arrest and apoptosis, and decreased survival of susceptible tumor cells. USP1, overexpressed in various tumor cell types, plays a key role in the correct folding and deubiquitylation of proteins and facilitates DNA repair via its role in regulating the Fanconi anemia complex and translesion synthesis. It plays an important role in the proliferation and survival of homologous repair deficiency (HRD)-positive tumor cells.
USP1 Inhibitor ISM3091
An orally bioavailable small molecule inhibitor of the human deubiquitinating enzyme ubiquitin specific protease 1 (USP1), with potential antineoplastic activity. Upon oral administration, USP1 inhibitor ISM3091 specifically targets, binds to and inhibits the activity of USP1, thereby blocking USP1-mediated deubiquitinating activity. This may result in replication fork degradation, inhibition of DNA damage repair, and decreased tumor cell survival. USP1, a deubiquitinating enzyme overexpressed in various tumor cell types, plays a key role in the correct folding and deubiquitylation of proteins and facilitates DNA repair via its role regulating the Fanconi anemia complex and translesion synthesis.
USP1 inhibitor KSQ-4279
An orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1), with apoptosis-inducing, tumor-sensitizing and antineoplastic activities. Upon oral administration, USP1 inhibitor KSQ-4279 specifically binds to and inhibits the activity of USP1, thereby blocking USP1-mediated deubiquitylating activity. This blocks the ubiquitin proteasome degradation pathway, prevents the degradation of defective proteins, and leads to an accumulation of mono-ubiquinated substrates. This induces the unfolded protein response (UPR). This may induce cell cycle arrest, reduce the expression of certain anti-apoptotic proteins, induce tumor cell apoptosis, inhibit tumor cell growth, and may sensitize tumor cells to DNA-targeting chemotherapeutics. USP1, a deubiquitinating enzyme overexpressed in various tumor cell types, plays a key role in the correct folding and deubiquitination of proteins and facilitates DNA repair via its role regulating the Fanconi anemia complex and translesion synthesis.
USP1 inhibitor SIM0501
An orally bioavailable non-covalent small molecule inhibitor of the human deubiquitinating enzyme ubiquitin specific protease 1 (USP1; ubiquitin carboxyl-terminal hydrolase 1), with potential antineoplastic activity. Upon oral administration, USP1 inhibitor SIM0501 specifically targets, binds to and inhibits the activity of USP1, thereby blocking complex formation of USP1 with USP1-associated factor 1 (UAF1), and inhibits USP1-mediated deubiquitinating activity. This may result in replication fork degradation, accumulation of mono-ubiquinated substrates, inhibition of DNA damage repair, induction of cell cycle arrest and apoptosis, and decreased survival of susceptible tumor cells. USP1, overexpressed in various tumor cell types, plays a key role in the correct folding and deubiquitylation of proteins and facilitates DNA repair via its role in regulating the Fanconi anemia complex and translesion synthesis. It plays an important role in the proliferation and survival of homologous repair deficiency (HRD)-positive tumor cells.
USP1 inhibitor TNG348
An orally bioavailable small molecule inhibitor of the human deubiquitinating enzyme ubiquitin specific protease 1 (USP1), with potential antineoplastic activity. Upon oral administration, USP1 inhibitor TNG348 specifically targets, allosterically binds to and inhibits the activity of USP1, thereby blocking USP1-mediated deubiquitinating activity. This may result in replication fork degradation, inhibition of DNA damage repair, and decreased tumor cell survival. USP1, a deubiquitinating enzyme overexpressed in various tumor cell types, plays a key role in the correct folding and deubiquitylation of proteins and facilitates DNA repair via its role regulating the Fanconi anemia complex and translesion synthesis. It plays a key role in the proliferation and survival of homologous recombination deficient (HRD)-positive tumor cells.
USP14/UCHL5 inhibitor VLX1570
An inhibitor of the 19S proteasome-specific deubiquitylating enzymes (DUBs) USP14 and UCHL5, with apoptosis-inducing and antineoplastic activities. Upon administration, VLX1570 specifically binds to both USP14 and UCHL5, thereby blocking their deubiquitylating activity. This blocks the ubiquitin proteasome degradation pathway, prevents the degradation of defective proteins, and leads to an accumulation of poly-ubiquitylated proteins. This induces the unfolded protein response (UPR) and results in both the induction of tumor cell apoptosis and the inhibition of tumor cell growth. USP14 and UCHL5, overexpressed in various tumor cell types, play a key role in the correct folding and deubiquitination of proteins.
ustekinumab
An orally available, human, IgG1kappa, monoclonal antibody directed against the p40 protein subunit of both interleukin-12 (IL-12) and IL-23, with immunomodulating activity. Upon administration, ustekinumab binds to the p40 subunit of IL-12 and IL-23, blocking the binding of IL-12 and IL-23 to their interleukin receptors. This inhibits IL-12- and IL-23-mediated signaling and inhibits differentiation of CD4 positive T-cells into Th1 and Th17 cells. This prevents Th1- and Th17-mediated responses and cytokine production. This may prevent graft versus host disease (GVHD). IL-12 and IL-23, cytokines that play a key role in the regulation of the immune system, are upregulated in immune-mediated inflammatory disorders. Both Th1 and Th17 cells play a crucial role in GVHD.
utatrectinib
A tropomyosin receptor kinase (TRK) inhibitor with potential antineoplastic activity. Upon administration, utatrectinib binds to TRK, thereby preventing the neurotrophin-TRK interaction and subsequent TRK activation. This may eventually result in an inhibition of tumor cell proliferation in TRK-expressing tumor cells. TRK, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth, invasion and survival.
utidelone
A genetically engineered epothilone analog with potential antineoplastic activity. Upon administration, utidelone binds to tubulin, induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and enhanced activity against certain multidrug-resistant (MDR) tumors.
Utimox
(Other name for: amoxicillin)
UV1 telomerase peptide vaccine
A synthetic, peptide cancer vaccine directed against the human telomerase reverse transcriptase catalytic subunit (hTERT) with potential immunomodulating activity. Vaccination with the UV1 telomerase peptide may stimulate cytotoxic T-cells to recognize and kill telomerase-expressing cells. Telomerase, a reverse transcriptase normally repressed in healthy cells, is overexpressed in most cancer cells and plays a key role in cellular proliferation.
Uvadex
(Other name for: methoxsalen)
Uvidem
(Other name for: autologous dendritic cell-allogeneic melanoma tumor cell lysate vaccine)
uzansertib
An orally available, small molecule and selective ATP-competitive pan-inhibitor of proviral integration sites for Moloney murine leukemia virus (PIM) kinases, with potential antineoplastic activity. Upon oral administration, uzansertib binds to and inhibits the activities of the three PIM isoforms, PIM1, PIM2 and PIM3. This prevents phosphorylation of their downstream targets and inhibits proliferation in cells that overexpress PIMs. PIMs, constitutively active proto-oncogenic serine/threonine kinases upregulated in various types of cancers, play key roles in tumor cell proliferation and survival.