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18:58 EST 20th February 2020 | BioPortfolio

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Showing PubMed Articles 1–25 of 79 from Expert opinion on investigational drugs

Combination therapies currently under investigation in phase I and phase II clinical trials for HIV-1.

: HIV infection is manageable through the use of antiretroviral drugs. However, HIV reservoirs that are constituted early during infection are resistant to treatment. HIV persistence under treatment necessitates life-long treatment and is associated with various co-morbidities. Two significant research avenues are explored through the development of either new antiretroviral drugs or interventions aimed at stimulating the immune system to eradicate HIV reservoirs. : This report provides a review of investig...

Investigational Drugs in Phase II Clinical Trials for Acute Coronary Syndromes.

: Despite current guideline-based, secondary prevention strategies in patients with the acute coronary syndrome, the residual ischemic risk is still at an unacceptable rate, and there is a concomitant high bleeding event rate. These observations mandate investigations of novel treatment strategies to meet the unmet need to improve outcomes in patients with ACS.: In this review, the author(s) focus on new agents with ongoing or recently completed phase II trials for the treatment of ACS. We searched MEDLINE ...

Etripamil nasal spray: an investigational agent for the rapid termination of paroxysmal supraventricular tachycardia (SVT).

: Paroxysmal supraventricular tachycardia (SVT) can be very bothersome and may potentially lead to considerable health-care utilization. Non-parenteral medication is currently unavailable for the rapid termination of paroxysmal SVT. However, an intranasal spray formulation of etripamil, a short-acting calcium-channel blocker, is under investigation as a convenient, safe, and rapidly efficacious means to terminate paroxysmal SVT.: This review summarizes the clinical rationale, potential benefit, and clinical...

Personalized pharmacological therapy for ARDS: a light at the end of the tunnel.

: Pharmacotherapy for the acute respiratory distress syndrome (ARDS) has been tested in preclinical and clinical studies. However, to date, no pharmacological interventions have proven effective. This may be attributed to lack of proper identification of different ARDS phenotypes.: We designed inclusive search strings and searched four bibliographic databases (Cochrane Database of Systematic Reviews, PubMed, Web of Science, and clinicaltrials.gov) to identify relevant research. Search results were mainly re...

Tyrosine kinase inhibitors for the treatment of rheumatoid arthritis: phase I to Ⅱ clinical trials.

: Rheumatoid arthritis (RA) is a chronic, refractory disorder caused by autoimmunity in the synovial joints. Disease-modifying anti-rheumatic drugs (DMARDs) and biologicals offer remission in only two-thirds of RA patients within 3 months, hence new therapeutic approaches are necessary. Tyrosine kinase inhibitors (TKIs) are newly developed small molecule drugs which have demonstrated encouraging results in this disease.: The key findings from phase I and II clinical trials that have investigated the use of ...

Insights into HIV-1 capsid inhibitors in preclinical and early clinical development as antiretroviral agents.

Investigational drugs for the treatment of binge eating disorder (BED): an update.

: Binge eating disorder (BED) is the most common eating disorder and is frequently associated with psychiatric and medical comorbidities and functional impairment. Although psychological treatments have been the cornerstones of BED treatment, pharmacologic interventions also play an important part of the multimodal management of this condition.: This review examines investigational, approved and other pharmacological agents for the treatment of BED. We searched PubMed and clinicaltrials.gov to identify phar...

Investigational BACE inhibitors for the treatment of Alzheimer's disease.

: The amyloid hypothesis of Alzheimer's disease (AD) states that brain accumulation of amyloid-β (Aβ) oligomers and soluble aggregates represents the major causal event of the disease. Several small organic molecules have been synthesized and developed to inhibit the enzyme (β-site amyloid precursor protein cleaving enzyme-1 or BACE1) whose action represents the rate-limiting step in Aβ production.: We reviewed the pharmacology and clinical trials of major BACE1 inhibitors.: In transgenic mouse models o...

Clinical drug development for dementia with Lewy bodies: past and present.

: Dementia with Lewy bodies (DLB) is an under-researched area despite being the second most common type of degenerative dementia after Alzheimer's disease. It is an area of unmet need with no approved symptomatic or disease-modifying therapies. The pharmacological management of DLB is complex and challenging because early trials of drugs for DLB have resulted in no demonstrable efficacy. Randomized controlled trials (RCTs) in the DLB population have only recently been initiated. Understanding results from p...

Tezepelumab: a novel biological therapy for the treatment of severe uncontrolled asthma.

: Thymic stromal lymphopoietin (TSLP) is overexpressed in the airways of severe asthmatics and is an upstream cytokine that orchestrates inflammatory responses in asthma. TSLP exerts its effects by binding to a high affinity heteromeric receptor complex composed of TSLPR and IL-7Rα. An association of polymorphisms in TSLP with airway hyperresponsiveness, IgE, eosinophilia and asthma has been documented. TSLP has been implicated in asthma pathophysiology. Tezepelumab is a first-in-class human monoclonal ant...

Tie-2/Angiopoietin pathway modulation as a therapeutic strategy for retinal disease.

: The Tie-2/Angiopoietin pathway is therapeutic target in neovascular age-related macular degeneration (nAMD) and diabetic macular edema (DME). Activation of Tie-2 receptor via Ang-1 maintains vascular stability to limit exudation. Ang-2, a competitive antagonist to Ang-1, and VE-PTP, an endothelial-specific phosphatase, interfere with the Tie-2-Ang-1 axis, resulting in vascular leakage. : Faricimab, a bispecific antibody that inhibits VEGF-A and Ang-2, is in phase 3 trials for nAMD and DME. Nesvacumab is a...

Defining and targeting wild-type BRCA high-grade serous ovarian cancer: DNA repair and cell cycle checkpoints.

: Molecular analyses including molecular descriptor/phenotype interactions have led to better characterization of epithelial ovarian cancer patients, including a definition of a BRCA wild-type (BRCAwt) phenotype. Understanding how and when to use agents targeted against dependent BRCAwt pathways or other molecular events at disease progression is an important translational and therapeutic direction in ovarian cancer research. : In this overview, we provide definitions and descriptions of a BRCAwt genotype a...

Acetyl-CoA carboxylase (ACC) as a therapeutic target for metabolic syndrome and recent developments in ACC1/2 inhibitors.

: Acetyl-CoA Carboxylase (ACC) is an essential rate-limiting enzyme in fatty acid metabolism. For many years, ACC inhibitors have gained great attention for developing therapeutics for various human diseases including microbial infections, metabolic syndrome, obesity, diabetes, and cancer. : We present a comprehensive review and update of ACC inhibitors. We look at the current advance of ACC inhibitors in clinical studies and the implications in drug discovery. We searched ScienceDirect ( https://www.scienc...

TTP399: an investigational liver-selective glucokinase (GK) activator as a potential treatment for type 2 diabetes.

Introduction Type 2 diabetes is a complex metabolic disorder defined by hyperglycemia which occurs because of impaired insulin secretion and sensitivity. There is a ongoing need to develop novel therapies that are effective and safe with minimal side effects and long-term durability. TTP399 is a hepatoselective, glucokinase activator with potential for treating type 2 diabetes. Areas covered This is a review of the available data regarding the mechanism of action and the pharmacokinetics of TTP399. The effi...

Investigative drugs for the treatment of cutaneous T-cell lymphomas (CTCL): an update.

: Cutaneous T-cell lymphoma (CTCL) is a heterogeneous group of skin-homing T-cell neoplasms, which represent approximately 75% of all primary cutaneous lymphomas. Mycosis fungoides and Sézary syndrome are the most common CTCL. Early stage disease follows a protracted course, carries a 5-year disease specific survival of 97% and can be treated with skin-directed therapies. Widespread, advanced disease has a 5-year OS of less than 25% and necessitates systemic treatment. Allogeneic stem cell transplantation ...

Prospects for the introduction of targeted antioxidant drugs for the prevention and treatment of diseases related to free radical pathology.

: Oxidative stress toxicity (OST) has been implicated in almost all pathological conditions. Despite the widespread use of natural antioxidants, no pharmaceutical antioxidants have yet been developed or prescribed in medical practise. Antioxidant drugs such as Deferiprone and N-acetylcysteine can target essential pathways of OST in many pathological conditions. The pharmacological parameters required by antioxidant drugs in relation to the OST target characteristics include the determination of the therapeu...

Gepants for the treatment of migraine.

Migraine is the most common of all neurological disorders. A breakthrough in migraine treatment emerged in the early nineties with the introduction of 5-HT1B/D receptor agonists called triptans. Triptans are used as the standard of care for acute migraine; however, they have significant limitations such as incomplete and inconsistent pain relief, high rates of headache recurrence, class- specific side effects and cardiovascular contraindications. First- and second-generation calcitonin gene-related peptide ...

Dasatinib as an investigational drug for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia in adults.

Acute lymphoblastic leukemia (ALL) with BCR-ABL1 translocation is an aggressive malignancy that is usually treated with intensive chemotherapy with the possibility of allogeneic stem cell transplantation. The encoded fusion protein may be important for leukemogenesis; clinical studies show that dasatinib has an antileukemic effect in combination with steroids alone or intensive chemotherapy. Areas covered. Relevant publications were identified through literature searches (the used terms being acute lymphobl...

Expert opinion on interleukin-12/23 and interleukin-23 antagonists as potential therapeutic options for the treatment of inflammatory bowel disease.

Blockade of interleukin (IL)-12 and IL-23 is a novel therapeutic target for inflammatory bowel disease (IBD). The monoclonal antibody targeting the shared p40 subunit of IL-12 and IL23, namely ustekinumab, has been approved for Crohn's disease (CD) and has demonstrated promising results in treatment of ulcerative colitis. Several agents targeting the IL-23-specific p19 subunit are currently in various stages of development. These newer agents have the potential to provide safety benefits. Areas covered: Thi...

Therapy of acute myeloid leukemia: therapeutic targeting of tyrosine kinases.

Tyrosine kinases (TKs) drive cell survival and proliferation in many normal and malignant cell types. TKs are frequently mutated in acute myeloid leukemia (AML) and hence are increasingly targeted. The management of AML has dramatically improved because of TKI-targeted treatment. Areas Covered: This review provides a biological background for TK inhibitors (TKIs) in AML and reviews their use in the clinic. TK expression and mutation in AML are explored with a focus on TKs associated with specific AML subset...

Investigational drug therapies currently in early stage clinical development for the treatment of clostridioides (clostridium) difficile infection.

Clostridioides (Clostridium) difficile Infection (CDI) is an urgent global threat causing ~500,000 infections annually in the United States of America (USA) and is associated with a 36% 30-day attributable mortality rate. Despite the availability of three therapeutic agents, CDI recurrence occurs in 20-40% of patients, with a 30-40% second recurrence rate in these patients. Consequently, there is a need for novel agents for treating CDI. Areas covered: We searched MEDLINE, PubMed, Embase, Web of Science, Co...

Investigational multitargeted kinase inhibitors in development for head and neck neoplasms.

Despite advances in treatment, head and neck squamous cell carcinoma (HNSCC) survival rates remain stagnant. Current treatment is associated with significant toxicities and includes chemotherapy, radiation, surgery and few targeted treatments. Targeted treatments, epidermal growth factor receptor (EGFR)-targeted agent, cetuximab, and immune checkpoint inhibitors, pembrolizumab and nivolumab, show improved toxicity profiles and modestly improved survival in select patients. An urgent need remains to identify...

Oral investigational drugs currently in phase I or phase II for the amelioration of menopausal symptoms.

Menopausal symptoms have a substantial effect on the quality of life of many women, hence investigations for the amelioration of menopausal symptoms continue to be necessary. The two main approaches to the amelioration of symptoms are hormone therapy (HT) and non-hormonal therapy. Areas covered: This review provides a background for understanding the types of menopausal symptoms and their underlying physiology. The early clinical development of a natural estrogen (estetrol, E4), neurokinin 3 receptor (NK3R)...

Investigational luteinizing hormone releasing hormone (LHRH) agonists and other hormonal agents in early stage clinical trials for prostate cancer.

The treatment and management of prostate cancer continues to evolve; newer classes of agents and combination therapies are being developed and some are being investigated in early phase clinical trials. Areas covered: We discuss investigational hormonal agents for the treatment of prostate cancer and focus primarily on luteinizing hormone releasing hormone (LHRH) agonists in early stage trials. We look at agents that target the hormonal axis, including anti-androgens, gonadotropins, estrogenic agents and pr...

An update of cyclooxygenase (COX)-inhibitors in epilepsy disorders.

Neuroinflammation has a critical role in brain disorders. Cyclooxygenase (COX) is one of the principal drug targets for the reduction of neuroinflammation; however, studies have yielded mixed results for COX-inhibitors in the treatment of diverse acute and chronic models of epilepsy. Areas covered: The article covers the effects of COX-inhibitors in epilepsy disorders. A considerable emphasis has been placed on the antiepileptic and "disease-modifying" properties of COX-1 and COX-2 inhibitors in various pre...


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