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Drug Dictionary


pan-FGFR tyrosine kinase inhibitor BAY1163877

A pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. Pan-FGFR kinase inhibitor BAY1163877 inhibits the activities of FGFRs, which may result in the inhibition of both tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. FGFRs are a family of receptor tyrosine kinases, which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-FGFR tyrosine kinase inhibitor JNJ-42756493

An orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Upon oral administration, JNJ-42756493 binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways and thus the inhibition of tumor cell proliferation and tumor cell death in FGFR-overexpressing tumor cells. FGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival. Check for active clinical trials using this agent.

Panglobulin

(Other name for: therapeutic immune globulin)

Panhematin

(Other name for: therapeutic hemin)

pan-HER kinase inhibitor AC480

An orally bioavailable, small-molecule pan-HER tyrosine kinase inhibitor with potential antineoplastic and radiosensitizing activities. Pan-HER kinase inhibitor AC480 binds to and inhibits the human epidermal growth factor receptors (HER) HER1 (EGFR), HER2 (ErbB-2) and HER4, which may prevent downstream signaling and inhibit the proliferation of tumor cells that overexpress these receptors. In addition, this agent may enhance the radiosensitivity of certain tumor cell types that express HER1 and HER2 through cell cycle redistribution in G1 phase and inhibition of DNA repair. EGFRs, frequently overexpressed on tumor cells, play a key role in tumor cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-HER/VEGFR2 receptor tyrosine kinase inhibitor BMS-690514

A pyrrolotriazine-based compound and a pan inhibitor of receptor tyrosine kinases with potential antineoplastic activity. Pan HER/VEGFR2 receptor tyrosine kinase inhibitor BMS-690514 binds to human epidermal growth factor receptors (EGFR) 1, 2 and 4 (HER1, HER2 and HER4) and vascular endothelial growth factor receptor 1, 2 and 3 (VEGFR-1, -2 and -3), all of which are frequently overexpressed by a variety of tumor types. Binding of this agent to these receptors may result in the inhibition of tumor cell proliferation; the inhibition of endothelial cell migration and proliferation and angiogenesis; and tumor cell death. Check for active clinical trials using this agent. (NCI Thesaurus)

panitumumab

A human monoclonal antibody produced in transgenic mice that attaches to the transmembrane epidermal growth factor (EGF) receptor. Panitumumab may inhibit autocrine EGF stimulation of tumor cells that express the EGF receptor, thereby inhibiting tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

panitumumab-IRDye800

An imaging agent composed of panitumumab, a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, conjugated to the near-infrared (NIR) fluorescent dye IRDye800, that can potentially be used for the imaging of EGFR-expressing tumors. Upon administration of panitumumab-IRDye800, the panitumumab moiety targets and binds to EGFR expressed on tumor cells. Upon fluorescence imaging of IRDye800, the tumor cells can be detected. Check for active clinical trials using this agent. (NCI Thesaurus)

PankoMab-GEX

(Other name for: anti-TA-MUC1 monoclonal antibody PankoMab)

panobinostat

A cinnamic hydroxamic acid analogue with potential antineoplastic activity. Panobinostat selectively inhibits histone deacetylase (HDAC), inducing hyperacetylation of core histone proteins, which may result in modulation of cell cycle protein expression, cell cycle arrest in the G2/M phase and apoptosis. In addition, this agent appears to modulate the expression of angiogenesis-related genes, such as hypoxia-inducible factor-1alpha (HIF-1a) and vascular endothelial growth factor (VEGF), thus impairing endothelial cell chemotaxis and invasion. HDAC is an enzyme that deacetylates chromatin histone proteins. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-PI3K inhibitor CLR457

An orally bioavailable pan inhibitor of phosphatidylinositol-3-kinase (PI3K), with potential antineoplastic activity. Upon oral administration, pan-PI3K inhibitor CLR457 inhibits all of the PI3K kinase isoforms, which may result in apoptosis and growth inhibition in tumor cells overexpressing PI3K. Activation of the PI3K pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-PI3K/mTOR inhibitor PQR309

An orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PQR309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy. As mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K, this agent may potentially be more potent than an agent that inhibits either PI3K kinase or mTOR kinase. By inhibiting mTOR to a lesser extent than PI3K, PQR309 does not interfere with the mTOR-mediated negative feedback loop on PI3K signaling. Blocking the negative feedback loop would potentially increase PI3K signaling and decrease therapeutic efficacy. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-PI3K/mTOR inhibitor SF1126

A water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities. The targeting peptide SF1174 moiety of pan-PI3K/mTOR inhibitor SF1126 selectively binds to cell surface integrins and, upon cell entry, the agent is hydrolyzed to the active drug SF1101; SF1101 selectively inhibits all isoforms of phosphoinositide-3-kinase (PI3K) and other members of the PI3K superfamily, such as the mammalian target of rapamycin (mTOR) and DNA-PK. By inhibiting the PI3K signaling pathway, this agent may inhibit tumor cell and tumor endothelial cell proliferation and survival.Integrins are transmembrane cell adhesion proteins expressed on the surfaces of endothelial and tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-PIM inhibitor INCB053914

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, pan-PIM kinase inhibitor INCB053914 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. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-PIM kinase inhibitor AZD1208

An orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity. Pan-PIM kinase inhibitor AZD1208 inhibits the activities of PIM1, PIM2 and PIM3 serine/threonine kinases, which may result in the interruption of the G1/S phase cell cycle transition, thereby causing cell cycle arrest and inducing apoptosis in cells that overexpress PIMs. The growth inhibition of several leukemia cell lines by this agent is correlated with the expression levels of PIM1, which is the substrate of STAT transcription factors. PIM kinases are downstream effectors of many cytokine and growth factor signaling pathways and are upregulated in various malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-Raf inhibitor LXH254

An orally available inhibitor of all members of the serine/threonine protein kinase Raf family, with potential antineoplastic activity. Upon administration, pan-RAF inhibitor LXH254 binds to Raf proteins and inhibits Raf-mediated signal transduction pathways. This inhibits proliferation of Raf-overexpressing tumor cells. Raf protein kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are upregulated in a variety of cancer cell types. They play key roles in tumor cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-RAF inhibitor LY3009120

An orally available inhibitor of all members of the serine/threonine protein kinase Raf family, including A-Raf, B-Raf and C-Raf protein kinases, with potential antineoplastic activity. Upon administration, pan-RAF kinase inhibitor LY3009120 inhibits Raf-mediated signal transduction pathways, which may inhibit tumor cell growth. Raf protein kinases play a key role in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK) signaling pathway, which is often dysregulated in human cancers and plays a key role in tumor cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-RAF kinase inhibitor CCT3833

An orally available inhibitor of the serine/threonine protein kinase family Raf, including A-Raf, B-Raf and C-Raf, with potential antineoplastic activity. Upon administration, pan-RAF kinase inhibitor CCT3833 inhibits Raf-mediated signal transduction pathways, which may inhibit the proliferation of Raf-overexpressing tumor cells. Raf protein kinases play a key role in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK) signaling pathway, which is often dysregulated in human cancers and plays a key role in tumor cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

pan-RAF kinase inhibitor TAK-580

An orally available inhibitor of A-Raf, B-Raf and C-Raf protein kinases, with potential antineoplastic activity. Upon administration, pan-RAF kinase inhibitor TAK-580 inhibits Raf-mediated signal transduction pathways, which may inhibit tumor cell growth. Raf protein kinases play a key role in the RAF/MEK/ERK signaling pathway, which is often deregulated in human cancers and plays a key role in tumor cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

Panretin

(Other name for: alitretinoin)

pan-selectin antagonist GMI-1070

A synthetic, glycomimetic molecule and pan-selectin antagonist, with potential use in a vaso-occlusive crisis. Upon administration, GMI-1070 prevents the interaction between leukocytes and the endothelium and may prevent cell activation and adhesion. By preventing selectin-mediated cell adhesion in sickle cell anemia, this agent may inhibit red blood cell-white blood cell interactions, normalize blood flow and reduce inflammation and vascular occlusive pain. GMI-1070 has the strongest antagonistic activity towards E-selectin but the incorporation of a sulfate-binding domain allows for interactions with P- and L-selectins. Selectins, containing lectin- and EGF-like domains, are a family of cell adhesion molecules implicated in inflammatory processes and cancer. Check for active clinical trials using this agent. (NCI Thesaurus)

pantoprazole sodium

The sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+/K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production. Check for active clinical trials using this agent. (NCI Thesaurus)

PANVAC-F

(Other name for: falimarev)

PANVAC-V

(Other name for: inalimarev)

pan-VEGFR/Tie2 tyrosine kinase inhibitor CEP-11981

An orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR) and Tie2 receptor tyrosine kinases with potential antiangiogenic and antineoplastic activities. Pan-VEGFR/Tie2 tyrosine kinase inhibitor CEP-11981 selectively binds to VEGFR and Tie2 receptor tyrosine kinases, which may result the inhibition of endothelial cell migration, proliferation and survival and the inhibition of tumor cell proliferation and tumor cell death. VEGFR and Tie2 are frequently overexpressed by a variety of tumor cell types and play crucial roles in the regulation of angiogenesis and the maintenance of tumor blood vessels. Tie2 (tyrosine kinase with immunoglobulin-likeand EGF-like domains) is activated by angiopoietin-1 (Ang-1). Check for active clinical trials using this agent. (NCI Thesaurus)

Panwarfin

(Other name for: warfarin)

Panzem

(Other name for: 2-methoxyestradiol)

papaverine

An opiate alkaloid isolated from the plant Papaver somniferum and produced synthetically. As a direct-acting smooth muscle relaxant, papaverine is not closely related to the other opium alkaloids in structure or pharmacological actions; its mechanism of action may involve the non-selective inhibition of phosphodiesterases and direct inhibition of calcium channels. This agent also exhibits antiviral activity against respiratory syncytial virus, cytomegalovirus, and HIV. Check for active clinical trials using this agent. (NCI Thesaurus)

Paraflex

(Other name for: chlorzoxazone)

Paraplat

(Other name for: carboplatin)

Paraplatin

(Other name for: carboplatin)

parathyroid hormone-related protein (1-36)

A recombinant form of a mature, N-terminal secretory peptide derived from a parathyroid hormone-related protein (PTHrP) preprohormone through posttranslational endoproteolytic processing with vasodilating, myorelaxant, and parathyroid hormone (PTH)-like calciotropic activities. Expressed throughout the cardiovascular system, parathyroid hormone-related protein (1-36) [PTHrP (1-36)] was first identified as the PTH-like hypercalcemic factor of humoral hypercalcemia of malignancy; however, its sequence differs significantly from that of PTH (1-34) although both proteins share the same N-terminal end which accounts for the calciotropic activity. Both PTHrP (1-36) and PTH (1-34) bind to the type 1 parathyroid hormone receptor (PTH1R), a specific seven-transmembrane-helix-containing G protein-coupled receptor mainly located in bone and kidney cells. Check for active clinical trials using this agent. (NCI Thesaurus)

parecoxib sodium

A water-soluble, injectable sodium salt form of parecoxib, an amide prodrug of the cyclooxygenase II (COX-2) selective, non-steroidal anti-inflammatory drug (NSAID) valdecoxib, with anti-inflammatory, analgesic, and antipyretic activities. Upon intravenous or intramuscular administration, parecoxib is hydrolyzed by hepatic carboxyesterases to its active form, valdecoxib. Valdecoxib selectively binds to and inhibits COX-2. This prevents the conversion of arachidonic acid into prostaglandins, which are involved in the regulation of pain, inflammation, and fever. This NSAID does not inhibit COX-1 at therapeutic concentrations and, therefore, does not interfere with blood coagulation. Check for active clinical trials using this agent.

paricalcitol

A synthetic noncalcemic, nonphosphatemic vitamin D analogue. Paricalcitol binds to the vitamin D receptor and has been shown to reduce parathyroid hormone (PTH) levels. This agent also increases the expression of PTEN ('Phosphatase and Tensin homolog deleted on chromosome Ten'), a tumor-suppressor gene, in leukemic cells and cyclin-dependent kinase inhibitors, resulting in tumor cell apoptosis and tumor cell differentiation into normal phenotypes. Check for active clinical trials using this agent. (NCI Thesaurus)

Parlodel

(Other name for: bromocriptine mesylate)

Parnate

(Other name for: tranylcypromine sulfate)

paromomycin sulfate

The sulfate salt form of paromomycin, a structural derivative of neomycin, an aminoglycoside antibiotic with amebicidal and bactericidal effects against predominantly aerobic gram-negative bacteria. Paromomycin binds specifically to the RNA oligonucleotide at the A site of bacterial 30S ribosomes, thereby causing misreading and premature termination of translation of mRNA and inhibition of protein synthesis followed by cell death. Check for active clinical trials using this agent. (NCI Thesaurus)

paroxetine hydrochloride

The hydrochloride salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties. Paroxetine binds to the pre-synaptic serotonin transporter complex resulting in negative allosteric modulation of the complex thereby blocking reuptake of serotonin by the pre-synaptic transporter. Inhibition of serotonin recycling enhances serotonergic function through serotonin accumulation in the synaptic cleft, resulting in long-term desensitization and downregulation of 5HT1 (serotonin) receptors and leading to symptomatic relief of depressive illness. Check for active clinical trials using this agent. (NCI Thesaurus)

PARP 1/2 inhibitor E7449

An orally available small molecule inhibitor of the nuclear enzymes poly (ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon administration, E7449 selectively binds to PARP 1 and 2, thereby preventing the repair of damaged DNA via the base excision repair (BER) pathway. This agent enhances the accumulation of single and double strand DNA breaks and promotes genomic instability eventually leading to apoptosis. PARP 1/2 inhibitor E7449 may enhance the cytotoxicity of DNA-damaging agents and of radiotherapy. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA. Check for active clinical trials using this agent. (NCI Thesaurus)

PARP inhibitor BGB-290

An orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP), with potential antineoplastic activity. PARP inhibitor BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. PARP is activated by single-strand DNA breaks and, subsequently, catalyzes post-translational ADP-ribosylation of nuclear proteins which then transduce signals to recruit other proteins to repair damaged DNA. BGB-290 may both potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo- and radioresistance. Check for active clinical trials using this agent. (NCI Thesaurus)

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