Ic50 dose response relationship drug. Medical search. Frequent questions

All dose-response curves plateaued at a certain LSD1 inhibitor concentration (Supplementary Fig. 2B ). (nature.com)
Dose-response relationships can be described by dose-response curves. (wikipedia.org)
Dose response relationships modelled by dose response curves are used extensively in pharmacology and drug development. (wikipedia.org)
citation needed] Statistical analysis of dose-response curves may be performed by regression methods such as the probit model or logit model, or other methods such as the Spearman-Kärber method. (wikipedia.org)
Logarithmic dose-response curves are generally sigmoidal-shape and monotonic and can be fit to a classical Hill equation. (wikipedia.org)
In contrast, nonspecifically binding compounds did not quench its fluorescence and showed similar IC(50) values with steep dose-response curves. (uzh.ch)
In this investigation, the cytotoxicity of 20 α-methylene-γ-lactones towards normal breast epithelial MCF-10A cells as well as breast cancer JIMT-1 cells is compared, by determining the inhibitory concentration 50 (IC50) from dose response curves. (lu.se)
Characterize your hits in dose-response curves. (samditech.com)
However, response curves for methotrexate were unsatisfactory and for paclitaxel, the solubilizer cremophor EL was toxic. (biomedcentral.com)
The problem is that smell is not quantifiable the way the effect of a drug is, through quantitative dose-response curves. (fieldofscience.com)

The Hill equation is the following formula, where E {\displaystyle E} is the magnitude of the response, [ A ] {\displaystyle {\ce {[A]}}} is the drug concentration (or equivalently, stimulus intensity) and E C 50 {\displaystyle \mathrm {EC} _{50}} is the drug concentration that produces a 50% maximal response and n {\displaystyle n} is the Hill coefficient. (wikipedia.org)
A commonly used dose-response curve is the EC50 curve, the half maximal effective concentration, where the EC50 point is defined as the inflection point of the curve. (wikipedia.org)
Transitions to the desensitized states by low concentration 'pre-pulses' are predicted to occur without significant channel opening, but equilibrium values of IC50 can be obtained only with long pre-pulse times. (unige.ch)
The lc50ld50 represent the concentration lc50 or dose ld50 at which. (web.app)
the concentration for half-inhibition (IC50) was 11 microM. (unboundmedicine.com)
It is essential to predict the effect on blood TAC concentration and manage drug interactions when both drugs are administered. (biomedcentral.com)
Red points are the median of the data sets for each drug concentration (N = 324), and green point is median in DMSO. (elifesciences.org)
The thrombin clotting time (TT) and ecarin clotting time (ECT) are highly sensitive to plasma melagatran concentrations (IC 50 approximately 0.01 micromol/L and approximately 0.15 micromol/L, respectively), with an approximate linear relationship between plasma melagatran concentration and prolongation of clotting time. (mcmaster.ca)
In comparison, the activated partial thromboplastin time (APTT) (IC 50 approximately 0.3 to 0.8 micromol/L) and prothrombin time (PT) (IC 50 approximately 0.9 to 2.9 micromol/L) are relatively insensitive, and the concentration-response relationship shows a flattening with increasing plasma melagatran concentration. (mcmaster.ca)
Sample analysis was performed on a FACSCanto II (BD Biosciences) with DIVA 8 software and histograms were generated using FlowJo v9 cytometry analysis software (Tree Star, Inc.). BRD inhibition/binding assays and profiling The half maximal inhibitory concentration (IC50) of each compound against BETs was determined by Reaction Biology Corp. using a chemiluminescent Alpha screen binding assay. (antiviralbiologic.com)
All drugs inhibited cell growth in a concentration-dependent manner with an IC50 comparable to that achievable in vivo . (biomedcentral.com)
was completed in healthful volunteers.ZYAN1 was safe and sound and well-tolerated in healthy volunteers following single escalating mouth dosages (10C300?mg) and multiple (particular once every 2?times) escalating mouth dosages (100C300?mg).Without consider to single or multiple oral dose administration, both mean maximum concentration ((AUCis portrayed under normoxic baseline conditions while is apparently a key aspect in the hypoxic response. (ap26113.com)
The datawere plotted as V versus V S, exactly where V would be the velocity from the response at a provided substrate concentration, and fitted to a straight line applying linear regression examination,the place the slope on the line corresponds toKm along with the Y intercept represents the Vmax. (vegfrinhibitors.com)

The clinical development of ximelagatran for the treatment and prevention of various arterial and venous thromboembolic disorders has used fixed-dose regimens without coagulation monitoring in all indications. (mcmaster.ca)
The success of complex antiretroviral regimens is dependent on consistent adherence of patients to the drugs. (who.int)
HA060 trade name] provides a combination of drugs i.e. lamivudine and zidovudine, that are already established as a backbone of the triple drug regimens. (who.int)

Both inhibitors decrease the proliferation of BC cell lines within a dose-dependent style (Fig. 2) with IC50 beliefs in the reduced micromolar range (Desk 3), recommending that dual mTOR inhibitors could be effective remedies for BC. (m2cobalt.com)
Open in another home window Fig. 2 Dual mTOR inhibitors inhibit bladder tumor cell growth within a dose-dependent way. (m2cobalt.com)
All human H5N1 isolates tested belonged to a single clade and were resistant to the adamantane drugs but sensitive to neuraminidase inhibitors. (cdc.gov)
Outcomes structure-activity and Style romantic relationship research of dual BET-kinase inhibitors BRDs and kinases are functionally and structurally unrelated, as well as the respective KAc and ATP binding sites will vary in architecture uniquely. (antiviralbiologic.com)
Monitor QT interval more frequently when RETEVMO is concomitantly administered with strong and moderate CYP3A inhibitors or drugs known to prolong QTc interval. (nih.gov)
The drugs for treatment of HIV infection are categorized as nucleoside reverse transcriptase inhibitors (NRTIs), protease inhibitors (PIs) and non- nucleoside reverse transcriptase inhibitors (NNRTIs). (who.int)
HA060 trade name] is a generic version of Combivir®, the first fixed-dose combination containing two known antiretroviral agents belonging to the RT inhibitors class. (who.int)

The non-linear relationship between cytotoxicity and dosage points toward proliferation arrest and differentiation in response to LSD1 inhibition. (nature.com)
These results revealed a potent proliferation block and induction of differentiation in non-DS-AMKL and ML-DS samples, however, the therapeutic efficacy of LSD1 inhibition may be limited by its non-linear dose-response relationship. (nature.com)
We conclude that almitrine inhibits selectively the Ca 2+ -dependent K + channel and that in rat chemoreceptor cells, this inhibition could represent an important mechanism of action underlying the therapeutic actions of the drug. (aspetjournals.org)
The diphosphate (dFdCDP) and triphosphate (dFdCTP) forms of the drug play an important role in the cytotoxic effect: dFdCDP is an inhibitor of ribonucleotide reductase, while dFdCTP is incorporated into DNA, both leading to the inhibition of DNA synthesis. (biomedcentral.com)
What is the necessary target compound profile (e.g. target engagement IC50, cellular growth inhibition GI50, and pharmacokinetics profile) to outcompete in direct and indirect competitions? (letsgobeyond.co.uk)
In this review, we summarize the current status and emerging trends in nanomedicine-based strategies targeting cancer immune evasion and modulating the immunosuppressive tumor microenvironment, including the inhibition of immunosuppressive cells in the tumor area, the activation of dendritic cells and the stimulation of the specific antitumor T-cell response. (unav.edu)
The extract also showed a dose dependent growth inhibition of all tested cell lines, IC 50 values against HCT-116, HUVEC, CCD-18CO and HT-29 were 14, 23, 50 and 52 μg mL -1 , respectively. (scialert.net)
Gene-drug level of sensitivity analyses and medication combination studies reveal synergism of BRD4 and kinase inhibition like a plausible reason behind the superior strength in cell eliminating. (antiviralbiologic.com)
Materials and Strategies Dataset This paper is dependant on the published evaluations of IC50 ideals dependant on AstraZeneca researchers [19], [20] (Fig 1) for inhibition against the Ephrin type-B receptor 4 (EphB4), a membrane-bound receptor tyrosine kinase that binds to ephrin-B2 ligands destined to the areas of additional cells to induce angiogenic occasions. (careersfromscience.org)
During in vitro evaluation in HepG2 cells, ZYAN1 demonstrated HIF stabilization by inhibiting the PHD enzyme (focus of drug generating 50% inhibition [IC50]: 11.2?mol/L) [24]. (ap26113.com)

Structure-activity relationships that may explain the observed differences in potency and selectivity are discussed. (lu.se)
Although the data in this field are not decisive and there are some confounding factors in human studies, it can be inferred that the use of any illicit drug with an effect on male sexual health reduces fertility potency. (magiran.com)
Future work will examine the variability of potency estimates, measured as the dose per skin area that sensitizes one subject. (nih.gov)

Generally speaking, the IC50 ideals produced using tip-based serial dilution and dispensing have a tendency to become higher (i.e., display lower strength) than IC50 ideals produced using acoustic dispensing. (careersfromscience.org)
Open up in another window Shape 1 The EphB4 IC50 ideals created via acoustic transfer with immediate dilution are considerably lower (even more biologically energetic) than when generated with tip-based transfer and serial dilutions.The ratio of the EphB4 IC50 values varies widely and correlates poorly using the calculated logP from the compounds (see also Desk S1). (careersfromscience.org)

Typical experimental design for measuring dose-response relationships are organ bath preparations, ligand binding assays, functional assays, and clinical drug trials. (wikipedia.org)
What is the best clinical dosing schedule for an optimal therapeutic window? (letsgobeyond.co.uk)
Despite the current revolutionary advances in the field of cancer immunotherapy, clinical response in breast cancer is frequently below expectations, in part due to various mechanisms of cancer immune escape that produce tumor variants that are resistant to treatment. (unav.edu)
The problems standing between the in vitro successes in antibiotic discovery laboratories and the clinical success of these drugs largely cluster around the drugs' poor pharmacokinetic profiles [1]. (biologists.com)
To this end, Laurie et al aim to repurpose drugs in current clinical use that already have favourable pharmacokinetic profiles to treat granulomatous amoebic encephalitis (GAE). (biologists.com)
The rationale is that, given that the library of drugs are already in clinical use, they would already have been studied-the pharmacology would be well characterised and the toxicities widely reported. (biologists.com)
However, this preprint is promising both in the discovery of a candidate in filling the gap that patients desperately need, as well as in showing how the strategy of drug repurposing is useful in urgent clinical needs where time is lacking, such as the field of antimicrobials. (biologists.com)
Clinical response to ASCT has been associated with DNA repair efficiency. (haematologica.org)
In the last two decades several integrin-targeted drugs have made their way into clinical use, many others are in clinical trials and still more are showing promise as they advance through preclinical development. (thno.org)
The Part 2 post in this series is concerned with mainline anti-cancer drug interventions that simultaneously address multiple growth pathways, ones that are entering clinical practice. (anti-agingfirewalls.com)

These data support the premise that HCN channels are valid targets for anti-depressive drugs albeit with a narrow therapeutic index. (frontiersin.org)
Drugs with higher HCN subtype selectivity are needed to establish if a wider therapeutic window can be obtained. (frontiersin.org)
Many medicinal plants have been directly used as the raw drug and these medicinal plants possess various therapeutic values. (ijpsonline.com)
1 Despite significant therapeutic advances for MM, autologous stem cell transplant (ASCT) following high-dose, single-agent melphalan conditioning remains a cornerstone of therapy. (haematologica.org)
5 This data proves an urgent need to identify biomarkers of de novo response and resistance to ASCT in order to improve patient selection for this therapeutic modality. (haematologica.org)
Patients are evaluated to determine the lowest dosage that produces a therapeutic response. (rxlist.com)

Various preclinical studies have investigated the effect of CBD on feeding behaviour in rodents [58, 93, 155,159,195], with results suggesting that higher doses may influence food intake several hours post-treatment. (researchgate.net)
The preclinical pharmacokinetic data indicated that ZYAN1 is usually well-absorbed and extremely bioavailable BSF 208075 after dental dosing over the varieties tested. (ap26113.com)

A structure-activity-relationship (SAR) study suggests that a metal binding mechanism for the original nitroxoline compound responsible for its antimicrobial activity. (biologists.com)

Plasma concentrations were well above the IC50 of several MMPs at all doses tested. (eur.nl)
All drugs were tested at the plasma concentrations achievable in vivo . (biomedcentral.com)

Further, this study elucidated the cellular and molecular mechanisms of nanoparticles for anti-proliferative and apoptotic effects on human lung cancer cells (A549) and compared them with commercial drug cisplatin. (springeropen.com)
Genomic polymorphism can influence drug transport, metabolism and cellular response, and lead to individual variations in terms of the response and toxicity and even to overall survival [ 8 , 9 ]. (biomedcentral.com)
Ca2+/calmodulin-dependent protein kinase II (CAMKII), multifunctional serine/threonine kinases, is a crucial mediator of translating intracellular Ca 2+ signals into cellular responses [ 6 ]. (aging-us.com)

A number of studies have investigated the relationships between treatment outcomes and individual genetic polymorphisms which will determine the efficacies and toxicities of chemotherapeutic agents, especially of 5-FU and platinum agents. (biomedcentral.com)
Desk 1 Statistical evaluation outcomes for correlations with IC50. (careersfromscience.org)

Studying dose response, and developing dose-response models, is central to determining "safe", "hazardous" and (where relevant) beneficial levels and dosages for drugs, pollutants, foods, and other substances to which humans or other organisms are exposed. (wikipedia.org)

In polyherbal medicine, medicinal plants with lower doses are strongly recommended to prevent side effects and achieve the necessary pharmacological activity[ 4 ]. (ijpsonline.com)
The physiological blood-brain barrier often presents a challenge to medicinal chemists and drug formulators in delivering the effective drugs to the brain where the infection resides. (biologists.com)

What Drugs, Substances, or Supplements Interact with Parlodel? (rxlist.com)

We report on phylogenetic, phenotypic, and antigenic analysis of H5N1 viruses from the 2004-2005 outbreak, focusing on these 3 genes, to address questions relevant to the public health response to the outbreak: 1) What is the genetic diversity of H5N1 viruses involved in human infections? (cdc.gov)

Nirmatrelvir/ritonavir is a potent cytochrome P450 (CYP) 3A inhibitor and influences pharmacokinetics of co-administered drugs. (biomedcentral.com)

The IC50 values in the two cell lines were found to depend on the overall structure of the assayed compounds, although less in this subset of compounds compared to a previous investigation. (lu.se)
One month after a single intravenous dose of rApoAI-PBGDms, the protein was still detectable in the liver, and hepatic PBGD activity remained increased above control values. (unav.edu)

Does variability in a tumour model from both in-house and published sources change the Exposure-Target Engagement-Disease Modulation/Physiological Response-Outcome relationship? (letsgobeyond.co.uk)

A dose-response curve is a coordinate graph relating the magnitude of a dose (stimulus) to the response of a biological system. (wikipedia.org)
How can i calculate ic50 using graph pad prism software. (web.app)

Cisplatin is commonly used to treat cervical cancer while drug resistance limits its effectiveness. (biomedcentral.com)
Laurie et al selected two glial cell lines, as well as those which represent the liver and kidney in which drug toxicities commonly manifest. (biologists.com)
For this purpose, ten HNSCC cell lines were tested for chemosensitivity against seven cytostatic drugs commonly used in the clinic, namely CIS, CPT, 5-FU, methotrexate (MTX), bleomycin (BLM), vincristine (VCR), and paclitaxel (PTX). (biomedcentral.com)

Cisplatin is a chemotherapy drug used to treat several cancer types such as bladder cancer, head and neck cancer, esophageal cancer, lung cancer, mesothelioma, brain tumors, and neuroblastoma. (springeropen.com)
With nearly a decade of experience with drug discovery, I have gained deep understanding in cancer treatments (radiation therapy, chemotherapy, targeted therapy, cancer immunotherapy) and DMPK (human PK prediction for small and large molecules, PBPK), I have helped pharmaceutical clients successfully advance their drug discovery projects into the clinics. (letsgobeyond.co.uk)
However, drug-resistance interferes with the effectiveness of chemotherapy. (biomedcentral.com)

The applied dose is generally plotted on the X axis and the response is plotted on the Y axis. (wikipedia.org)

In drug discovery, the occurrence of false positives is a major hurdle in the search for lead compounds that can be developed into drugs. (uzh.ch)
Raltitrexed and Safinamide act as potent repurposed drugs, and three other Specs database compounds using in silico methods. (bvsalud.org)
Herein, this review examines and evaluates the various drugs and compounds targeting integrins and the disease states in which they are implicated. (thno.org)

Prism 6 stepbystep example analyzing doseresponse data in pharmacology experiments, a drugs effect on a receptor is typically investigated by constructing a doseresponse curve. (web.app)
Graphpad prism was originally designed for experimental biologists in medical schools and drug companies, especially those in pharmacology and physiology. (web.app)

2016 ). This study was conducted to analyze the anticancer effects of green-synthesized AgNPs using Juniperus polycarpos on A549 (adenocarcinomic human alveolar basal epithelial cells) cell lines, as well as comparing it with Cisplatin commercial drug. (springeropen.com)
OSI-027 and PP242 diminish cell proliferation in every 3 cell lines with IC50 beliefs which range from 0.63 to 17.95 M. Both drugs inhibit phosphorylation of both mTORc2 and mTORc1 pathway components. (m2cobalt.com)
One cell range exhibited apoptosis in response to mixture medications, whereas the various other 2 cell lines possess increased degrees of autophagy indicative of level of resistance to apoptosis. (m2cobalt.com)
Dose-response experiments with various cell lines to represent important physiologic organs (fibroblast, glial cells, kidney, and liver) and both mandrillaris trophozites and cysts revealed that nitroxoline may even be superior to existing drugs used in the standard of care for GAE in two ways. (biologists.com)

Wistar rats) [155], failed to influence food intake during a 1 h ad libitum feeding period, moderate to high doses of CBD (4.4 mg·kg −1 , i.p. [58]. (researchgate.net)

In particular, the shape of a drug's dose-response curve (quantified by EC50, nH and ymax parameters) reflects the biological activity and strength of the drug. (wikipedia.org)

Responses can be recorded as continuous data (e.g. force of muscle contraction) or discrete data (e.g. number of deaths). (wikipedia.org)
Empirical models based on nonlinear regression are usually preferred over the use of some transformation of the data that linearizes the dose-response relationship. (wikipedia.org)
Prism 6 stepbystep example analyzing doseresponse data. (web.app)
Black line is the Hill equation fit to the median data by a nonl-inear fitting algorithm (IC50 = 115.4, Hill coefficient = −1.71). (elifesciences.org)
dose-response data (IC50 = 133.4, Hill coefficient = −1.47). (elifesciences.org)
For discovery and development of novel cancer treatments, this means vagueness in tumour model data interpretation and poses challenges for robust decision making in drug discovery & development. (letsgobeyond.co.uk)
The purpose of this review was to collect as much literature as possible about the impact of illicit drugs on male fertility and summarize their valuable data. (magiran.com)

Both propolis extracts exhibited high anti-HSV-1 activity when the viruses were pretreated with these drugs prior to infection. (nih.gov)
2) Can the relationship between human and avian H5N1 isolates help explain the source of infection? (cdc.gov)
The standard of care in Human Immunodeficiency Virus (HIV) infection is the use of a triple drug antiretroviral regimen. (who.int)

In particular, many solid-organ transplant patients are on tacrolimus (TAC) therapy, a substrate drug for CYP3A4/5. (biomedcentral.com)

Evaluate structure activity relationship (SAR) and identify critical moieties for optimal target engagement. (samditech.com)
Sub-optimal adherence may reduce the effectiveness of the regimen by allowing viral replication and the emergence of drug resistant strains. (who.int)

However, a structure-activity relationship study that ensued did not yield more potent leads. (uzh.ch)
There are many cases wherein multiple drugs inhibit CYP activity. (biomedcentral.com)
The negative relationship between C-CDK activity and cell growth refers to the block of cell length extension in mitosis. (elifesciences.org)
have reported anti-carcinogenic activity of both koetjapic acid and 3-oxo-olean-12-en-29-oic acid. (scialert.net)
The evaluation of the biogenic amine steady state level is currently considered a useful tool to predict the effect of a drug on the activity in the brain, particularly in in vivo studies [44,45]. (researchgate.net)
2 The primary driver of response to ASCT is the depth of anti-myeloma activity of melphalan. (haematologica.org)

However, prognosis of MM still remains unsatisfactory with most patients experiencing drug resistance or early relapse [ 5 ]. (aging-us.com)

The adage The dose makes the poison reflects how a small amount of a toxin has no significant effect, while a large amount may be fatal. (wikipedia.org)
Drug combinations often give rise to a promising effect in treatment of diseases over a single drug[ 1 ]. (ijpsonline.com)

Integrin-mediated interactions with the extracellular matrix (ECM) are required for the attachment, cytoskeletal organization, mechanosensing, migration, proliferation, differentiation and survival of cells in the context of a multitude of biological processes including fertilization, implantation and embryonic development, immune response, bone resorption and platelet aggregation. (thno.org)

Almitrine is a drug used in the treatment of hypoxemic chronic lung diseases such as bronchitis and emphysema because it is a potent stimulant of the carotid bodies in human and different animal species that produces a long-lasting enhancement of alveolar ventilation, ameliorating arterial blood gases. (aspetjournals.org)

Here we interrogated the role of the base excision DNA repair (BER) pathway in MM response to ASCT. (haematologica.org)

Zero relationship was discovered between tumor and staining stage. (m2cobalt.com)

The sensitivity of this assay makes it highly useful for hit finding and validation in drug discovery. (uzh.ch)
By using WES, we identified a frequently mutated locus SETD8 (7%), which was associated with drug sensitivity. (biomedcentral.com)

The U.S. Food and Drug Administration also has guidance to elucidate dose-response relationships during drug development. (wikipedia.org)
DDUNAV - Drug Development Unit of University of Navarra: Unidad de desarrollo preclínico: Responsable de estudios de farmacocinética y farmacocinética/farmacodinamia (Oct- 2015-actualidad) - Secretaría de la Junta del Departamento de Tecnología y Química Farmacéuticas. (unav.edu)
Typically, drug development first involves the identification of a target. (biologists.com)
The development of a fixed dose combination aims to reduce the number of daily tablets, and therefore enhance adherence to therapy and thereby minimizing the risk of emergence of resistance. (who.int)

These observations indicate the need to investigate mechanisms of drug resistance. (biomedcentral.com)
In order to overcome drug-resistance, the exploration of underlying mechanisms is necessary. (biomedcentral.com)

BSF 208075 The effective dosage for inducing hematopoiesis was noticed to become 15?mg/kg, with another dosing design for weekly. (ap26113.com)

Management of drug-drug interaction by pharmacists can be important for patients with multiple medications. (biomedcentral.com)

Continue steroids until patient reaches target dose and then taper. (nih.gov)

HA060 trade name] has a simple dosing schedule of one tablet, twice daily, with no food restrictions or water requirements. (who.int)

Drug combination treatments of cancer and infectious diseases have given patients new hope in current years[ 2 ]. (ijpsonline.com)
In particular, the discovery of the new use of artemisinin derivatives as excellent anti-cancer drugs is also reviewed. (anti-agingfirewalls.com)

It had been noticed that in single-dose research, ZYAN1 was tolerated up to 300?mg/kg in mice, up to 800?mg/kg in rats, or more to 75?mg/kg in beagle canines by the dental INHA route [24]. (ap26113.com)

It is not indicated for use in paediatric patients less than 12 years of age and patients with renal impairment, since it is a fixed dose combination that cannot e titrated for these patients. (who.int)

Therefore, it is recommended that couples, who are planning to conceive, avoid taking any illicit drugs before and during treatment. (magiran.com)
Consider available information on influenza drug susceptibility patterns and treatment effects when deciding whether to use. (nih.gov)
Systemic treatment of head and neck squamous cell carcinoma (HNSCC) includes a variety of antineoplastic drugs. (biomedcentral.com)

A stimulus response function or stimulus response curve is defined more broadly as the response from any type of stimulus, not limited to chemicals. (wikipedia.org)

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