An amino acid analogue and antibiotic derived from the bacterium Streptomyces alanosinicus with antimetabolite and potential antineoplastic activities. L-alanosine inhibits adenylosuccinate synthetase, which converts inosine monophospate (IMP) into adenylosuccinate, an intermediate in purine metabolism. L-alanosine-induced disruption of de novo purine biosynthesis is potentiated by methylthioadenosine phosphorylase (MTAP) deficiency. The clinical use of this agent may be limited by its toxicity profile. MTAP is a key enzyme in the adenine and methionine salvage pathways.
L-arginine/Korean ginseng/ Gingko biloba/damiana-based supplement
An amino acid and herbal supplement with libido-enhancing activity. L-arginine/korean ginseng/Ginkgo biloba/damiana-based supplement contains a blend of the amino acid L-arginine and the herbs Korean ginseng, Ginkgo biloba, and damiana (Turnera aphrodisiaca) in addition to 14 other vitamins and minerals. The semi-essential amino acid L-arginine is a precursor for nitric oxide (NO); Korean ginseng may enhance the conversion of L-arginine into NO by NO synthase; and Ginkgo biloba may promote microvascular circulation. This agent may increase NO production, resulting in vasodilatation and an enhanced circulation critical to sexual function and arousal. The damiana component may exert an anxiolytic effect and stimulate sexual behavior.
(Other name for: asparaginase)
L-Carnipure L-Carnitine L-Tartrate
(Other name for: L-carnitine L-tartrate)
A dietary supplement containing the levo-enantiomers of carnitine and tartrate with potential chemoprotective and antioxidant activities. L-carnitine L-tartrate increases fatty acid oxidation and reduces purine catabolism and free radical formation, which may prevent exercise fatigue, muscle weakness, chemotherapy-induced peripheral neuropathy, and hyperlipoproteinemia. L-carnitine, the biologically active form of carnitine, is a carrier molecule that transports activated long-chain fatty acids (LCFAs)from the cytosol to mitochondria where fatty acids are oxidized, resulting in ATP production,. L-tartrate, a salt of tartaric acid, is a potent antioxidant.
A non-essential amino acid. In hepatocytes, L-citrulline is synthesized in the urea cycle by the addition of carbon dioxide and ammonia to ornithine. L-citrulline is converted into L-arginine by the enzymes argininosuccinate synthetase and argininosuccinate lyase in the presence of L-aspartate and ATP. Subsequently, L-arginine is converted to nitric oxide by nitric oxide synthase and L-citrulline is regenerated as a by-product .
The levo-enantiomer of an orally bioavailable polyphenolic aldehyde, derived primarily from unrefined cottonseed oil, with potential antineoplastic activity. Mimicking the
inhibitory BH3 (Bcl-2 homology 3) domain of endogenous antagonists of Bcl-2, L-gossypol binds to and inhibits various anti-apoptotic Bcl-2 proteins, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. This agent has greater affinity for Bcl-2 proteins than racemic gossypol.
The active l-isomer of the racemic mixture of the 5-formyl derivative of tetrahydrofolic acid. Metabolically active, l-leucovorin, also known levoleucovorin, does not require bioactivation by dihydrofolate reductase, an enzyme inhibited by folic acid antagonists. This agent may enhance the effects of fluoropyrimidines by stabilizing their binding to the enzyme thymidylate synthase.
L-leucyl-L-leucine methyl ester
A 2-amino acid compound with immunomodulatory activity. L-leucyl-L-leucine methyl ester (LLME) is a lysosomotropic agent entering cells via receptor-mediated endocytosis. LLME undergoes a condensation process catalyzed by dipeptidyl peptidase I (DPPI) in lysosomes. Condensation of LLME leads to lysosomal rupture and DNA fragmentation in DPPI-expressing immune cells such as cytotoxic T-cells and natural killer cells. Therefore, this agent may be able to decrease the incidence of graft versus host disease (GVHD) via cytotoxic T-cell depletion. Furthermore, LLME has the potential for augmenting antibody production when used in pretreatment of peripheral blood mononuclear cells (PBMCs), possibly by interfering with gene expression of inflammatory factors.
A nutritional supplement containing the biologically active L-isomer of the essential amino acid lysine, with potential anti-mucositis activity. Upon oral intake, L-lysine promotes healthy tissue function, growth and healing and improves the immune system. L-Lysine promotes calcium uptake, is essential for carnitine production and collagen formation. As collagen is essential for connective tissue maintenance, this agent may also help heal mucosal wounds. This may help decrease and prevent mucositis induced by radiation or chemotherapy.
L19-IL2 monoclonal antibody-cytokine fusion protein
An immunoconjugate consisting of the recombinant form of the cytokine interleukin-2 (IL-2) fused to a human single-chain Fv (scFv) antibody fragment directed against the extra-domain B (ED-B) of fibronectin (L19), with potential immunopotentiating and antineoplastic activities. The L19 moiety of L19-IL2 monoclonal antibody-cytokine fusion protein binds to the ED-B domain of fibronectin on tumor cells in the tumor neovasculature. In turn, the IL-2 moiety may locally activate natural killer (NK) cells and macrophages, and may induce T cell cytotoxic immune responses against ED-B fibronectin-expressing tumor cells. This may specifically decrease the proliferation of ED-B-expressing tumor cells. ED-B is predominantly expressed during angiogenesis and tumor growth.
labetuzumab-SN-38 immunoconjugate IMMU-130
An antibody-drug conjugate (ADC) containing labetuzumab, a mildly reduced, anti-CEACAM5 humanized monoclonal antibody, conjugated to the potent topoisomerase I inhibitor SN-38, with antineoplastic activity. The monoclonal antibody moiety of antibody-drug conjugate IMMU-130 selectively binds to carcinoembryonic cell adhesion molecule 5 (CEACAM5), which is abundantly expressed on the surface of a majority of solid tumors. Upon internalization and proteolytic cleavage, SN-38, the active metabolite of irinotecan, inhibits the activity of topoisomerase I in the tumor cells, eventually inhibiting both DNA replication and transcription and leading to tumor cell apoptosis.
(Other name for: theophylline)
Lactobacillus acidophilus probiotic
A probiotic containing the bacterium Lactobacillus acidophilus with potential antimicrobial and immunomodulatory activities. As a dietary supplement, Lactobacillus acidophilus (L. acidophilus), a naturally-occurring bacteria, may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. Because it produces lactic acid and hydrogen peroxide and other substances during fermentation, this bacterium creates an acidic environment unfavorable to pathogens such as Candida albicans. In addition, during colonization of the GI tract, L. acidophilus may form a protective barrier, preventing attachment of pathogens. Dietary supplementation with this bacterium has been shown to enhance natural and acquired immunity in mice.
lactobacillus fermented extract
A proprietary dietary supplement. Lactobacillus fermented extract is made from soymilk fermented by several strains of lactobacillus and yeast via a symbiotic co-culturing technology. The composition of the agent includes amino acids, vitamins, minerals, fatty acids, isoflavones, and saponins. Lactobacillus fermented extract may support healthy intestinal function.
Lactobacillus plantarum strain 299
A nutritional supplement containing the probiotic bacterium Lactobacillus plantarum 299 (Lp 299) with potential antimicrobial, immune-boosting, and anti-inflammatory activities. Upon oral ingestion, Lp 299 adheres to the intestinal mucosa, modulates the composition of the normal microflora, helps maintain adequate colonization of the gastrointestinal (GI) tract and improves digestion and metabolism. Upon colonization of the GI tract, the probiotic may form a protective barrier, thereby preventing attachment of pathogens, protecting against infections and boosting the immune system. In addition, Lp 299 stimulates the secretion of protective mucin and produces lactic acid and hydrogen peroxide as well as other substances, thereby creating an acidic environment which prevents growth of pathogens.
Lactobacillus plantarum strain 299v
A nutritional supplement containing a strain of the probiotic bacterium Lactobacillus plantarum 299v (Lp 299v) with potential antimicrobial, immune-boosting, and anti-inflammatory activities. Upon oral ingestion, L. plantarum strain 299v adheres to the intestinal mucosa, modulates the composition of the normal microflora, helps maintain adequate colonization of the gastrointestinal (GI) tract and improves digestion and metabolism. Upon colonization of the GI tract, the probiotic may form a protective barrier, thereby preventing attachment of pathogens, protecting against infections and boosting the immune system. In addition, Lp 299v stimulates the secretion of protective mucin and produces lactic acid and hydrogen peroxide as well as other substances, thereby creating an acidic environment which prevents growth of pathogens.
lactoferrin-derived lytic peptide LTX-315
A peptide derived from human lactoferrin, with potential lytic and immunostimulating activities. Upon transdermal injection directly into the tumor, LTX315 may bind to the tumor cell membranes and subsequently lyse tumor cells, thereby inducing tumor cell necrosis. In turn, presentation of the tumor antigens to the immune system may induce systemic innate and adaptive immune responses mediated by anti-tumor natural killer (NK) cells, cytotoxic T lymphocytes, and natural killer T (NKT) cells. This may trigger an immune response against tumor associated antigens on tumors distant from the primary tumor. Human lactoferrin, a 692 amino acid glycoprotein, belongs to the transferrin family of metal-binding proteins.
(Other name for: lamotrigine)
lanreotide acetate copolymer microparticles
A prolonged-release depot suspension of microparticles containing the acetate salt of lanreotide, a synthetic peptide analog of the naturally occurring somatostatin, and copolymers. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent has a much longer duration of action than natural somatostatin and is selective towards the inhibition of growth hormone.
(Other name for: lanreotide long-acting aqueous gel)
lanreotide long-acting aqueous gel
A long-acting aqueous gel preparation of lanreotide, a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit the release of various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent also decreases circulating total and free insulin-like growth factor 1 (IGF-I). Lanreotide exhibits a high binding affinity for somatostatin receptor 2 (SSTR-2) and a lesser binding affinity for SSTR-5. However, compared to octreotide, this agent is less potent in inhibiting the release of growth hormone from the pituitary gland.
(Other name for: levodopa)
(Other name for: levodopa)
A semi-synthetic derivative of the taxane 10-deacetylbaccatin III with potential antineoplastic activities. Larotaxel binds to tubulin, promoting microtubule assembly and stabilization and preventing microtubule depolymerization, thereby inhibiting cell proliferation. As it represents poor substrate for P-glycoprotein-related drug resistance mechanisms, this agent may be useful for treating multi-drug resistant tumors. Larotaxel penetrates the blood brain barrier.
(Other name for: furosemide)
(Other name for: bimatoprost ophthalmic solution)
(Other name for: hydromorphone hydrochloride)
A glycosylated form of a recombinant therapeutic agent which is chemically identical to or similar to an endogenous human granulocyte colony-stimulating factor (G-CSF). Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions.
A synthetic, orally available inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR/FLK-1) tyrosine kinase with potential antineoplastic activity. Lenvatinib mesylate blocks VEGFR2 activation by VEGF, resulting in inhibition of the VEGF receptor signal transduction pathway, decreased vascular endothelial cell migration and proliferation, and vascular endothelial cell apoptosis.
(Other name for: fluvastatin sodium)
leucine-enhanced essential amino acid dietary supplement
An orally bioavailable leucine enriched essential amino acid dietary supplement with potential anti-cachexia activity. Leucine-enhanced essential amino acid nutritional supplement may stimulate the mammalian target of rapamycin (mTOR) signaling pathway, which may promote protein synthesis in muscle cells. Although the exact mechanism by which leucine and other essential amino acids stimulate mTOR has yet to be fully elucidated, leucine may stimulate mTOR by inhibiting adenosine monophosphate protein kinase (AMPK), which negatively controls mTOR signaling.
leukemic apoptotic corpse-pulsed autologous dendritic cells
A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with corpses of apoptotic leukemic cells, with potential immunostimulatory and antineoplastic activities. Upon vaccination, autologous dendritic cells pulsed with leukemic apoptotic corpse may activate the immune system to mount an anti-tumoral cytotoxic T-lymphocyte (CTL) response against leukemic cells expressing leukemia-associated antigens, which may result in leukemic cell lysis and inhibition of tumor cell growth. Apoptotic tumor cell corpses contain an array of tumor associated antigens (TAAs).
(Other name for: sargramostim)
(Other name for: cladribine)
The orally bioavailable hydrochloride salt of the synthetic imidazothiazole derivative levamisole with anthelminthic and immunostimulating activities. In immunosuppressed states, levamisole may restore immune function by: 1) stimulating antibody formation, 2) stimulating T-cell activation and proliferation, 3) potentiatiating monocyte and macrophage phagocytosis and chemotaxis and 4) increasing neutrophil mobility, adherence, and chemotaxis.
(Other name for: levofloxacin)
(Other name for: vardenafil hydrochloride)
An amino acid precursor of dopamine with antiparkinsonian properties. Levodopa is a prodrug that is converted to dopamine by DOPA decarboxylase and can cross the blood-brain barrier. When in the brain, levodopa is decarboxylated to dopamine and stimulates the dopaminergic receptors, thereby compensating for the depleted supply of endogenous dopamine seen in Parkinson's disease. To assure that adequate concentrations of levodopa reach the central nervous system, it is administered with carbidopa, a decarboxylase inhibitor that does not cross the blood-brain barrier, thereby diminishing the decarboxylation and inactivation of levodopa in peripheral tissues and increasing the delivery of dopamine to the CNS.
A synthetic cannabinoid analogue of delta (9)-tetrahydrocannabinol (delta(9)-THC) with antiemetic and anti-analgesic properties. Although its precise mechanism of action is unknown, levonantradol appears to bind and activate the cannabinoid receptors CB1 and/or CB2.
levonorgestrel-releasing intrauterine system
A long-acting, hormone-releasing, intrauterine device consisting of a small, T-shaped, polyethylene frame and a reservoired synthetic progesterone with progestational and potential antineoplastic activities. After insertion of this system into the uterus, the device slowly and gradually releases the hormone. Levonorgestrel acts by binding to the progesterone receptor in the nuclei of target cells, resulting in transcription activation and an alteration in protein synthesis. Subsequently, luteinizing hormone (LH) activity and ovulation are suppressed. Levonorgestrel may also exhibit antiproliferative activity in endometrial tissue.
(Other name for: levodopa)
The sodium salt of levothyroxine, a synthetic levoisomer of thyroxine (T4) that is similar to the endogenous hormone produced by the thyroid gland. In peripheral tissues, levothyroxine is deiodinated by 5'-deiodinase to form triiodothyronine (T3). T3 enters the cell and binds to nuclear thyroid hormone receptors; the activated hormone-receptor complex in turn triggers gene expression and produces proteins required in the regulation of cellular respiration; thermogenesis; cellular growth and differentiation; and the metabolism of proteins, carbohydrates and lipids. T3 also exhibits cardiostimulatory effects.
(Other name for: levothyroxine sodium)
An orally bioavailable small-molecule with tubulin-inhibiting, vascular-disrupting, and potential antineoplastic activities. Lexibulin inhibits tubulin polymerization in tumor blood vessel endothelial cells and tumor cells, blocking the formation of the mitotic spindle and leading to cell cycle arrest at the G2/M phase; this may result in disruption of the tumor vasculature and tumor blood flow, and tumor cell death.
The orally active fumarate salt of the benzimidazole derivative liarozole with potential antineoplastic activity. As a retinoic acid metabolism blocking agent (RAMBA), liarozole inhibits cytochrome P450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, resulting in an increase in endogenous ATRA production, inhibition of cell proliferation, and induction of cell differentiation. This agent also inhibits aromatase, the enzyme that catalyzes the final, rate-limiting step in estrogen biosynthesis.
(Other name for: liarozole fumarate)
(Other name for: fluocinonide cream)
lidocaine patch 5%
A transdermal patch containing a 5 percent aqueous base solution of the synthetic amide-type anesthetic lidocaine with analgesic activity. Upon topical application and transdermal delivery, the active ingredient lidocaine binds to and blocks voltage-gated sodium channels in the neuronal cell membrane; lidocaine-mediated stabilization of neuronal membranes inhibits the initiation and conduction of nerve impulses and produces a reversible local anesthesia.
(Other name for: lidocaine patch 5%)
(Other name for: lidocaine)
light-emitting oncolytic vaccinia virus GL-ONC1
An attenuated oncolytic vaccinia virus encoding the light-emitting fusion protein Renilla luciferase-Aequorea green fluorescent protein (RUC-GFP) with potential bioluminescent and antineoplastic activities. Upon administration, light-emitting oncolytic vaccinia virus GL-ONC1 specifically enters tumor cells due to the permeable nature of the tumor vasculature. Once inside the cell, the virus replicates, resulting in tumor cell lysis and the release of mature viral particles into the tumor microenvironment. Released viral particles may then infect and destroy neighboring tumor cells. In addition, the release of tumor-associated antigens (TAAs) by lysed tumor cells into the bloodstream may activate the immune system to mount a cytotoxic T lymphocyte (CTL) response against the tumor. The expression of RUC-GFP by this agent allows for both detection and monitoring of virally infected tumor cells in vivo and vitro with luciferase-mediated bioluminescence imaging and fluorescence imaging techniques.
An oral dietary supplement containing a natural cyclic monoterpene and major component of the oil extracted from citrus peels with potential chemopreventive and antitumor activities. Although the mechanism of action has yet to be fully elucidated, limonene and its metabolites perillic acid, dihydroperillic acid, uroterpenol and limonene 1,2-diol may inhibit tumor growth through inhibition of p21-dependent signaling and may induce apoptosis via the induction of the transforming growth factor beta-signaling pathway. In addition, they inhibit post-translational modification of signal transduction proteins, resulting in G1 cell cycle arrest as well as differential expression of cell cycle- and apoptosis-related genes.
(Other name for: chlorambucil)
An orally bioavailable, small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Linifanib inhibits members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families; it exhibits much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. This agent does not have a general antiproliferative effect due to its high dose requirement. However, linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as fms-related tyrosine kinase receptor-3 (FLT3).
(Other name for: roquinimex)
An orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGFR-1 stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.
(Other name for: ethiodized oil)
(Other name for: therapeutic progesterone)
liposomal amphotericin B
A liposome-encapsulated formulation of the polyene antifungal antibiotic amphotericin B produced by the bacterium Streptomyces nodosus with antifungal activity. Amphotericin B binds to ergosterol, an essential component of the fungal cell membrane, and alters cell membrane integrity, resulting in leakage of intracellular components and cell rupture. This agent may also induce oxidative damage in fungal cells and has been reported to stimulate host immune cells. Compared to amphotericin B alone, liposomal delivery of amphotericin B allows for a greater drug concentration in target tissues while decreasing systemic side effects.
A liposome-encapsulated form of the semi-synthetic doxorubicin analogue annamycin with antineoplastic activity. Annamycin intercalates into DNA and inhibits topoisomerase II, resulting in the inhibition of DNA replication and repair and RNA and protein synthesis. This agent circumvents multidrug-resistance (MDR) transporters, including P-glycoprotein (P-gp). Liposomal annamycin is less toxic and shows improved antitumor activity compared to annamycin.
A sterically stabilized, pegylated liposomal formulation containing CKD602, a semi-synthetic analogue of campthotecin with potential antitumor activity. CKD602 inhibits the action of topoisomerase I, an enzyme that produces reversible single-strand breaks in DNA during DNA replication. CDK602 stabilizes the topoisomerase I and DNA complex, resulting in the inhibition of religation of DNA breaks, inhibition of DNA replication, and apoptotic cell death. The polyethylene glycol coating of liposomal belotecan allows for greater plasma circulation time, thus enhancing the concentration of CKD602 at the tumor site. Encapsulation of CKD602 preserves the active lactone form, resulting in an increased cytotoxic effect of CKD602.
liposomal c-raf antisense oligonucleotide
The liposomal formulation of a c-raf-1 antisense oligonucleotide, with potential antineoplastic activity. Liposomal c-raf antisense oligonucleotide targets the translation initiation site of human c-raf-1 mRNA, thereby blocking the expression and production of Raf-1 protein and thus inhibits tumor cell growth and development. Raf-1 plays a key role in the RAF/MEK/ERK signaling pathway, which regulates mammalian cell proliferation and growth. The liposomal formulation increases the solubility of the c-raf antisense oligonucleotide, thus improving its pharmacodynamic profile.
A synthetic formulation in which the antineoplastic agent cisplatin is encapsulated in lipids. Liposomal cisplatin consists of small aggregates of cisplatin covered by a single lipid bilayer. Encasement in liposomes improves cisplatin's tumor bioavailability and toxicity profile. Liposomal encapsulation does not affect the pharmacological properties of cisplatin directly. Cisplatin forms highly reactive, charged, platinum complexes which bind to nucleophilic groups such as GC-rich sites in DNA, inducing intrastrand and interstrand DNA cross-links, as well as DNA-protein cross-links. These cross-links result in apoptosis and cell growth inhibition.
liposomal cytarabine-daunorubicin CPX-351
A liposomal formulation containing a fixed combination of the antineoplastic agents cytarabine and daunorubicin in a 5:1 molar ratio. Liposomal cytarabine-daunorubicin CPX-351 has been designed to provide optimal delivery of a specific ratio of cytarabine to daunorubicin, one that has been shown to be synergistic in vitro. The antimetabolite cytarabine competes with cytidine for incorporation into DNA, inhibiting DNA synthesis. This agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Daunorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in the cytotoxic lipid peroxidation of cell membrane lipids.
liposomal daunorubicin citrate
A liposome-encapsulated form of the citrate salt of the anthracycline antineoplastic antibiotic daunorubicin. Daunorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Liposomal delivery of doxorubicin citrate improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects.
A formulation of the poorly soluble, semi-synthetic, second-generation taxane docetaxel encapsulated within liposomes, with antineoplastic activity. Upon intravenous administration, docetaxel binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell-cycle arrest at the G2/M phase and cell death. This liposomal formulation solubilizes docetaxel without the use of toxic solvents such as Tween 80, permitting the administration of larger doses of docetaxel while avoiding solvent-associated toxicity, including hypersensitivity reactions. In addition, liposomal delivery of docetaxel improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects while lowering the toxicity profile.
A formulation in which liposomes are loaded with the cytokine interleukin-2 (IL-2). By activating cytotoxic T lymphocytes, such as lymphokine-activated killer cells, and increasing levels of the cytotoxic cytokines interferon-gamma (IFN-gamma) and transforming growth factor-beta (TGF-beta), IL-2 may exhibit antitumoral activity. Liposomal formulations of IL-2 may promote entry of the cytokine into target tumor cells and may be used as an immunoadjuvant in cancer vaccine therapy.
A liposome-encapsulated formulation of lurtotecan with antineoplastic activity. Lurtotecan, a semisynthetic analogue of camptothecin, selectively stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex during S phase of the cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-stranded DNA breaks. This ultimately results in an inhibition of DNA replication, inducing double-stranded DNA breakages, obstruction of RNA and protein synthesis and triggering apoptosis. Furthermore, this agent also stimulates degradation of topoisomerase I, likely mediated through ubiquitin-proteasomal pathway. Liposomal delivery of lurtotecan improves its penetration and delivery into tumors while lowering systemic side effects.
A synthetic liposomal formulation of bis-neodecanoate diaminocyclohexane platinum (NDDP), a third-generation platinum complex analogue of cisplatin, with potential antineoplastic activity. After displacement of the 2 long-chain aliphatic leaving groups (neodecanoic acid), platinum diaminocyclohexane (DACH) complexes become highly reactive and alkylate macromolecules, forming both inter- and intra-strand DNA crosslinks and inhibiting DNA synthesis, which results in tumor cell cytotoxicity. Because DNA mismatch-repair (MMR) complexes do not recognize DACH–platinum adducts, DNA repair mechanisms are inhibited, overcoming limitations observed with other platinum-based agents. In addition, the liposomal encapsulation improves the bioavailability of NDDP and reduces its toxicity profile.
A liposomal formulation of the prodrug oxaliplatin, an organoplatinum complex in which the platinum atom is complexed with 1,2-diaminocyclohexane (DACH) and with an oxalate ligand as a 'leaving group', with antineoplastic activity. After displacement of the labile oxalate ligand leaving group, the active oxaliplatin derivatives monoaquo and diaquo DACH platinum alkylate macromolecules, and form both inter- and intra-strand platinum-DNA crosslinks; inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity ensue. The DACH side chain appears to inhibit alkylating-agent resistance. A leaving group is an atom or a group of atoms that is displaced as a stable species taking with it its bonding electrons.
liposomal T4N5 lotion
A topical lotion that contains the enzyme T4-bacteriophage endonuclease V encapsulated within liposomes. With topical liposomal delivery, the DNA repair enzyme T4-bacteriophage endonuclease V is transported into skin cells, where the enzyme enters cell nuclei and binds to and incises pyrimidine dimers, thereby catalyzing the first reaction step of the cellular excision repair pathway for removing DNA replication-inhibiting pyrimidine dimers produced within duplex DNA through exposure to ultraviolet (UV) irradiation. In vitro and in vivo studies indicate that T4N5 liposomes increases repair of DNA damage caused by UV irradiation.
liposomal topotecan hydrochloride
The hydrochloride salt of a semisynthetic derivative of camptothecin mixed with sphingomyelin/cholesterol and sonicated to form small unilamellar vesicles containing topotecan, with potential antineoplastic activity. Liposomal opotecan hydrochloride mediates efficient drug delivery of topotecan into the cytosol from the endosome compartment. During the S phase of the cell cycle, topotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery.
An intravenous formulation of tretinoin (vitamin A acid or all-trans retinoic acid) encased in liposomes. Tretinoin is a naturally occurring retinoic acid agent that binds to and activates retinoic acid receptors (RAR), effecting changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of carcinogenesis. This agent also inhibits telomerase, leading to telomere shortening and eventual apoptosis of certain tumor cell types. Liposome encapsulation extends the half-life of intravenously administered tretinoin.
liposome-encapsulated irinotecan hydrochloride PEP02
A liposomal formulation of the hydrochloride salt of the semisynthetic camptothecin analogue irinotecan with potential antineoplastic activity. During the S phase of the cell cycle, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell.
liposome-incorporated Grb2 antisense oligodeoxynucleotide
A liposomal formulation containing the antisense oligodeoxynucleotide (ODN) growth factor receptor-bound protein 2 (Grb2), with potential antineoplastic activity. Upon administration, liposome-incorporated Grb2 antisense oligodeoxynucleotide binds directly to and blocks Grb2 mRNA, thereby preventing Grb2 protein synthesis, leading to inhibition of cell proliferation of cancer cells overexpressing Grb2. Grb2, an adaptor protein involved in growth signaling pathways, is upregulated in certain tumor cells.
(Other name for: camptothecin analogue TLC388)
The dimesylate form and prodrug of the d-isomer of amphetamine, a non-catecholamine sympathomimetic amine with central nervous system (CNS) stimulating activity. Upon administration, lisdexamphetamine is converted to dextroamphetamine through cleavage of the lysine group. Dextroamphetamine acts by facilitating the release of catecholamines, particularly noradrenaline and dopamine, from its storage sites in nerve terminals in the CNS, and inhibits their uptake within the mesocorticolimbic system, a major component of the brain reward system, resulting in measurable behavioral changes such as euphoria, mental alertness and excitement and appetite suppression. As a CNS stimulant, this agent may increase blood pressure.
(Other name for: lithium carbonate)
The carbonate salt of lithium, a soft alkali metal, with antimanic and hematopoietic activities. Lithium interferes with transmembrane sodium exchange in nerve cells by affecting sodium, potassium-stimulated adenosine triphosphatase (Na+, K+-ATPase); alters the release of neurotransmitters; affects cyclic adenosine monophosphate (cAMP) concentrations; and blocks inositol metabolism resulting in depletion of cellular inositol and inhibition of phospholipase C-mediated signal transduction. The exact mechanism through which lithium exerts its mood-stabilizing effect has not been established. In addition, lithium stimulates granulocytopoiesis and appears to increase the level of pluripotent hematopoietic stem cells by stimulating the release of hematopoietic cytokines and/or directly acting on hematopoietic stem
(Other name for: lithium carbonate)
(Other name for: lithium carbonate)
(Other name for: lithium carbonate)
An inhibitor of the kinesin-related motor protein Eg5 with potential antineoplastic activity. Litronesib selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and consequently cell death in tumor cells that are actively dividing. The ATP-dependent Eg5 kinesin-related motor protein (also known as KIF11 or kinesin spindle protein-5) is a plus-end directed kinesin motor protein that plays an essential role during mitosis, particularly in the regulation of spindle dynamics, including assembly and maintenance.
live attenuated measles virus vaccine
A live, attenuated measles vaccine with potential antineoplastic activity. Upon subcutaneous administration, live attenuated measles virus vaccine may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against measles-positive tumor cells. Measles virus has been shown to be present in some non-small cell lung cancers.
live freeze-dried lactic acid bacteria probiotic
A probiotic containing live, cultivated, freeze-dried lactic acid bacteria with gastrointestinal (GI) protective, anti-inflammatory, immunomodulating and potential antitumor properties. Oral administration of probiotic bacteria help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier, interfere with the attachment of pathogenic bacteria and other harmful substances and may bind to and degrade carcinogens. This may prevent inflammation and possibly cancer. In addition, these bacteria produce lactic acid, thereby creating an acidic environment that is unfavorable for pathogens.
live-attenuated Listeria encoding human mesothelin vaccine CRS-207
A recombinant Listeria-based cancer vaccine containing a live-attenuated strain of the facultative intracellular bacterium Listeria monocytogenes (Lm) expressing human mesothelin with potential immunostimulatory and antineoplastic activities. Upon administration of this vaccine, Listeria invade professional phagocytes within the immune system and express mesothelin, which may activate a cytotoxic T-lymphocyte (CTL) response against mesothelin-expressing tumor cells, resulting in tumor cell lysis. In addition, the Listeria vector itself may induce a potent innate and adaptive immunity unrelated to mesothelin expression. Mesothelin is a cell surface glycoprotein involved in cell adhesion and is overexpressed in many epithelial-derived cancers, including pancreatic, ovarian and lung cancers, and malignant mesotheliomas.
live-attenuated Listeria monocytogenes cancer vaccine ADXS11-001
A cancer vaccine containing a live-attenuated strain of the bacterium Listeria monocytogenes (Lm) encoding human papillomavirus (HPV) type 16 E7 fused to a non-hemolytic listeriolysin O protein with potential immunostimulatory and antineoplastic activities. Upon vaccination, Listeria expresses the HPV 16 E7 antigen and activates the immune system to mount a cytotoxic T-lymphocyte (CTL) response against cancer cells expressing HPV 16 E7. This may result in tumor cell lysis. In addition, the Listeria vector itself may induce a potent immune response. HPV 16 E7, a cell surface glycoprotein and tumor associated antigen, is overexpressed in the majority of cervical cancer cells.
LMP-2:340-349 peptide vaccine
A peptide cancer vaccine containing amino acid residues 340-349 of the Epstein-Barr virus (EBV) latent membrane protein-2 (LMP-2) with potential immunostimulating and antineoplastic activities. Vaccination with LMP-2:340-349 peptide may boost the immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against LMP-2-expressing tumor cells, resulting in cell lysis and inhibition of tumor cell proliferation. LMP-2, an EBV transmembrane protein, is expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease.
LMP-2:419-427 peptide vaccine
A peptide cancer vaccine containing amino acid residues 419-427 of the latent membrane protein-2 (LMP-2) of the Epstein-Barr virus (EBV) with potential immunostimulating and antineoplastic activities. Vaccination with the LMP-2:49-427 peptide vaccine may boost the immune system to mount a specific cytotoxic T-lymphocyte response against LMP-2-expressing tumor cells, resulting in cell lysis and inhibition of tumor cell proliferation. LMP-2, an EBV transmembrane protein, is expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease.
LMP2a-specific cytotoxic T-lymphocytes
A preparation of cytotoxic T-lymphocytes (CTL), specifically reactive to Epstein-Barr virus (EBV) latent membrane protein-2A (LMP2A), with potential antineoplastic activity. T-lymphocytes are exposed ex vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP2A. Subsequently, LMP2A-specific CTLs are exposed to EBV infected cells transfected with adenovirus encoding LMP2A, thereby further stimulating CTLs. Administered to patients with EBV-positive tumors, LMP2A-specific CTLs target LMP2A-positive cells, resulting in cell lysis and inhibition of cancer cell proliferation. EBV LMP2A may be expressed in various malignancies, including nasopharyngeal carcinoma and Hodgkin and non-Hodgkin lymphomas.
(Other name for: etodolac)
An orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity. Lonaprisan is a pure, highly receptor-selective progesterone receptor (PR) antagonist; binding of this agent to PRs inhibits PR activation and the associated proliferative effects. Unlike many other antiprogestins such as mifepristone, this agent does not appear to convert to an agonist in the presence of protein kinase A (PKA) activators and shows high antiprogestagenic activity on both progesterone receptor (PR) isoforms PR-A and PR-B.
(Other name for: ciclopirox olamine lotion)
(Other name for: hydrocodone/acetaminophen)
An immunoconjugate of a humanized murine monoclonal antibody (huN-901) and DMI, a semi-synthetic derivative of the plant-derived ansa macrolide maytansine. The antibody moiety of lorvotuzumab mertansine selectively attaches to CD56 antigen, a neural cell adhesion molecule (NCAM)) expressed on the surface of cells of small cell lung cancer (SCLC) and other neuroendocrine (NE) tumors. Thus, the DMI conjugate is targeted specifically to CD56-expressing tumor cells, where it inhibits tubulin polymerization and assembly, resulting in inhibition of mitosis and cell cycle arrest in the S phase.
(Other name for: benazepril hydrochloride)
(Other name for: clotrimazole)
(Other name for: live-attenuated Listeria monocytogenes cancer vaccine ADXS11-001)
(Other name for: enoxaparin)