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  • cytotoxicity
  • Anti-CD70 antibody-drug conjugates (ADC) consisting of auristatin phenylalanine phenylenediamine (AFP) or monomethyl auristatin phenylalanine (MMAF), two novel derivatives of the anti-tubulin agent auristatin, mediated potent antigen-dependent cytotoxicity in CD70-expressing RCC cells. (aacrjournals.org)
  • The efficiency of drug delivery using anti-CD70 as vehicle was illustrated by the much enhanced cytotoxicity of antibody-conjugated MMAF compared with free MMAF. (aacrjournals.org)
  • clinical
  • Please refer to CG-DRUG-64 FDA-Approved Biosimilar Products for additional information on clinical criteria for review of a biosimilar product to an already FDA-approved TNF antagonist (a biological product, known as the reference product) addressed in CG-DRUG-65. (unicare.com)
  • Recent clinical studies on several classes of experimental drugs, including small molecule inhibitors of protein kinases ( 14 - 16 ) and antibodies targeting vascular endothelial growth factor ( 17 ) or the RCC-associated antigen CAIX ( 18 ), have shown promise. (aacrjournals.org)
  • Once a compound that fulfills all of these requirements has been identified, it will begin the process of drug development prior to clinical trials. (wikipedia.org)
  • The drug requires very expensive Phase I, II and III clinical trials, and most of them fail. (wikipedia.org)
  • tumor cell
  • Hence, ADCs targeted to CD70 can selectively recognize RCC, internalize, and reach the appropriate subcellular compartment(s) for drug release and tumor cell killing. (aacrjournals.org)
  • leukemia
  • In our present study, 1200 off-patent marketed drugs and natural compounds that have been approved by the Food and Drug Administration (FDA) were screened for anti-leukemia activity using the retrovirus transduction/transformation assay (RTTA). (plos.org)
  • The introduction of all-trans retinoic acid (ATRA) to treat acute promyelocytic leukemia (APL), a subtype of acute myeloid leukemia (AML), pioneered a new approach to obtain remission in malignancies by restoring the terminal maturation of leukemia cells . (plos.org)
  • Acute myeloid leukemia (AML) is a hematological malignancy with poor prognosis, and therefore there is a pressing need to develop drugs with excellent activity and fewer toxic side effects . (plos.org)
  • Hairy cell leukemia typically shows high levels of CD22 expression but the drug also showed signs of activity in other indications, such as chronic lymphocytic leukemia. (aacrjournals.org)
  • activity
  • Especially, the paper focused on the relevant mechanism study of EAC-B against MGC-803 included cell cycle distribution (flow cytometry) and cyclin D1 expression (RT-PCR and western blot), apoptosis (Hoechst 33342 stain and flow cytometry), apoptosis-related protein expression (Akt, p-Akt, ERK, p-ERK, Bcl-2, Bax) by western blot, and caspase3/7 activity assay. (biomedcentral.com)
  • The idea that the effect of a drug in the human body is mediated by specific interactions of the drug molecule with biological macromolecules, (proteins or nucleic acids in most cases) led scientists to the conclusion that individual chemicals are required for the biological activity of the drug. (wikipedia.org)
  • Historically, substances, whether crude extracts or purified chemicals, were screened for biological activity without knowledge of the biological target. (wikipedia.org)
  • involves
  • Modern drug discovery is thus usually a capital-intensive process that involves large investments by pharmaceutical industry corporations as well as national governments (who provide grants and loan guarantees). (wikipedia.org)
  • Discovering drugs that may be a commercial success, or a public health success, involves a complex interaction between investors, industry, academia, patent laws, regulatory exclusivity, marketing and the need to balance secrecy with communication. (wikipedia.org)
  • biological
  • more aggressive use of conventional drugs, and biological targeted therapies have each made a significant impact. (ncl.ac.uk)
  • Despite advances in technology and understanding of biological systems, drug discovery is still a lengthy, "expensive, difficult, and inefficient process" with low rate of new therapeutic discovery. (wikipedia.org)
  • study
  • In this study, we screened a traditional Chinese medicine (TCM) compound library consisting of 800 single compounds in TKI-resistance NSCLC H1975 cells, which contains substitutions from leucine to arginine at amino acid 858 (L858R) and T790M mutation on EGFR. (mdpi.com)
  • effect
  • Meanwhile, for disorders whose rarity means that no large commercial success or public health effect can be expected, the orphan drug funding process ensures that people who experience those disorders can have some hope of pharmacotherapeutic advances. (wikipedia.org)
  • However
  • However, drug resistance frequently happens due to additional mutation on EGFR, such as substitution from threonine to methionine at amino acid position 790 (T790M). (mdpi.com)
  • additional
  • For additional information on review of clinically equivalent cost effective criteria for products addressed in CG-DRUG-65, please refer to CG-ADMIN-02 Clinically Equivalent Cost Effective Services - Targeted Immune Modulators . (unicare.com)
  • discovery
  • The significance of healing property herbs has been highly evaluated in drug discovery. (biomedcentral.com)
  • Historically, drugs were discovered through identifying the active ingredient from traditional remedies or by serendipitous discovery. (wikipedia.org)
  • Drug discovery is done by pharmaceutical companies, with research assistance from universities. (wikipedia.org)
  • doses
  • Linear PK was observed with doses ≥400 mg q2w indicating target-mediated drug disposition saturation. (aacrjournals.org)
  • natural
  • Fortunately, Paclitaxel (Taxol) is proved to be a successful drug extracted from natural product to answer the call to fill the need. (biomedcentral.com)
  • tests
  • Conventional CRC screening tests include fecal occult blood testing, flexible sigmoidoscopy, doublecontrast barium enema X-ray, and colonoscopy [ 3 ]. (omicsonline.org)
  • active
  • It should be noted that each 200 mg tablet contains only 155 mg of active drug. (medscape.com)
  • Examples of drug compounds isolated from crude preparations are morphine, the active agent in opium, and digoxin, a heart stimulant originating from Digitalis lanata. (wikipedia.org)
  • five
  • Among four fractions, the IC50s of n-BuOH fraction of EAC (EAC-B) against the five cell lines and time-dependent inhibition to gastric cancer cell line (MGC-803) were further investigated (MTT assay). (biomedcentral.com)
  • small
  • This project aims to repurpose a small molecule anti-cancer drug as an anti-fibroblast drug for RA. (ncl.ac.uk)
  • Later, small molecules were synthesized to specifically target a known physiological/pathological pathway, avoiding the mass screening of banks of stored compounds. (wikipedia.org)
  • process known
  • Mitomycin C (MMC) is a clinically used anticancer drug that is reduced to cytotoxic metabolites by cellular reductases via a process known as bioreductive drug activation. (aacrjournals.org)
  • Moreover
  • Moreover, these results establish that the IA determinants mediating cytotoxicity are precisely those that facilitate ABCG2-dependent drug efflux and IA resistance. (aspetjournals.org)
  • A patient with severe infection of staphylococcus aureus acquired completely spontaneous remission (SR), moreover a increased number of pDC were observed, suggesting that bacteria-activated pDC may play an important role in SR. This study was purposed to explore if the bacteria can stimulate pDC successfully and get a functional pDC. (jove.com)
  • compounds
  • Herein, this review examines and evaluates the various drugs and compounds targeting integrins and the disease states in which they are implicated. (thno.org)
  • These ATP-driven efflux pumps, which recognize a plethora of hydrophobic, hydrophilic and amphiphilic compounds, extrude out of malignant cells structurally distinct endo- and xenobiotics, many of which are key antitumor agents, thereby resulting in a wide spectrum of MDR. (aspetjournals.org)
  • Since sequencing of the human genome which allowed rapid cloning and synthesis of large quantities of purified proteins, it has become common practice to use high throughput screening of large compounds libraries against isolated biological targets which are hypothesized to be disease modifying in a process known as reverse pharmacology. (wikipedia.org)
  • Examples of drug compounds isolated from crude preparations are morphine, the active agent in opium, and digoxin, a heart stimulant originating from Digitalis lanata. (wikipedia.org)
  • Later, small molecules were synthesized to specifically target a known physiological/pathological pathway, avoiding the mass screening of banks of stored compounds. (wikipedia.org)
  • Patients
  • Optimal care of patients with rheumatoid arthritis (RA) requires an integrated approach that includes both nonpharmacologic therapies and pharmacologic agents such as nonbiologic and biologic disease-modifying antirheumatic drugs (DMARDs), nonsteroidal anti-inflammatory drugs (NSAIDs), analgesics, and corticosteroids. (medscape.com)
  • Conclusions PF-04236921 50 mg induced clinical response and remission in refractory patients with moderate-to-severe CD following failure of anti-TNF therapy. (bmj.com)
  • resistance
  • Taking advantage of the inherent fluorescent properties of IAs, ABCG2-dependent efflux and drug resistance were determined in A549/K1.5 cells using flow cytometry in the presence or absence of fumitremorgin C, a specific ABCG2 transport inhibitor. (aspetjournals.org)
  • Hence, the current study offers novel molecular insight into the structural determinants that facilitate ABCG2-mediated drug efflux and consequent drug resistance using a unique platform of fluorescent IAs. (aspetjournals.org)
  • rare
  • sub.2 -microglobulin cDNA clones: A screening procedure for cDNA clones corresponding to rare mRNAs," Proc. (patentgenius.com)
  • Spontaneous remission (SR) of leukemia is a rare event in clinic, which possibly correlated with severe infection and sepsis, but its exact mechanism has not been confirmed. (jove.com)
  • made
  • This made for the beginning of the modern era in pharmacology, as pure chemicals, instead of crude extracts of medicinal plants, became the standard drugs. (wikipedia.org)
  • cancer
  • In countries with screening programs, breast cancer is often detected before clinical symptoms are apparent, but occasionally the occurrence of a paraneoplastic syndrome precedes the identification of cancer. (biomedcentral.com)
  • Hence, the development of novel modalities that overcome ABCG2-dependent MDR phenomena in various human cancers is one of the major goals of current preclinical cancer therapeutics and an ongoing pursuit in the field of rational drug design. (aspetjournals.org)