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Items 1 to 10 of about 324640
1. Patterson JT, Isaacson J, Kerwin L, Atassi G, Duggal R, Bresson D, Zhu T, Zhou H, Fu Y, Kaufmann GF: PSMA-targeted bispecific Fab conjugates that engage T cells. Bioorg Med Chem Lett; 2017 Dec 15;27(24):5490-5495
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] PSMA-targeted bispecific Fab conjugates that engage T cells.
  • Bioconjugate formats provide alternative strategies for antigen targeting with bispecific antibodies.
  • Here, PSMA-targeted Fab conjugates were generated using different bispecific formats.
  • Interchain disulfide bridging of an αCD3 Fab enabled installation of either the PSMA-targeting small molecule DUPA (SynFab) or the attachment of an αPSMA Fab (BisFab) by covalent linkage.
  • Optimization of the reducing conditions was critical for selective interchain disulfide reduction and good bioconjugate yield.
  • Activity of αPSMA/CD3 Fab conjugates was tested by in vitro cytotoxicity assays using prostate cancer cell lines.
  • Both bispecific formats demonstrated excellent potency and antigen selectivity.

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  • [Copyright] Copyright © 2017. Published by Elsevier Ltd.
  • (PMID = 29126850.001).
  • [ISSN] 1464-3405
  • [Journal-full-title] Bioorganic & medicinal chemistry letters
  • [ISO-abbreviation] Bioorg. Med. Chem. Lett.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; Bioconjugation / Bispecific antibody / Click chemistry / Disulfide bridging / Fab
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2. Kong W, Romo D: Diastereo- and Enantioselective Synthesis of Bi- and Tricyclic N-Heterocycle-Fused β-Lactones. J Org Chem; 2017 Dec 15;82(24):13161-13170

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Diastereo- and Enantioselective Synthesis of Bi- and Tricyclic N-Heterocycle-Fused β-Lactones.
  • The utility of the nucleophile-catalyzed (Lewis base) aldol lactonization (NCAL) process for the diastereo- and enantioselective synthesis of N-heterocycle-fused-β-lactones from N-linked ketoacids is described.
  • A series of bi- and tricyclic, N-heterocycle-fused, β-lactones were first synthesized in racemic fashion via the NCAL process with excellent diastereoselectivity (>19:1) utilizing 4-pyrrolidinopyridine as an effective achiral Lewis base.
  • A catalytic, enantioselective version of this NCAL process using isothiourea catalysts provided access to bicyclic β-lactone-fused, N-heterocycles in moderate to good yields (up to 80%) with high enantiocontrol (up to >99:1 er).
  • An unusual diastereodivergent NCAL process was discovered that leads to two different products; a tricyclic N-heterocycle-fused β-lactone and a bicyclic enamine derived from in situ decarboxylation of the diastereomeric tricyclic β-lactone.
  • The reactivity of these adducts was briefly explored.

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  • (PMID = 29125760.001).
  • [ISSN] 1520-6904
  • [Journal-full-title] The Journal of organic chemistry
  • [ISO-abbreviation] J. Org. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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3. White AM, Dao K, Vrubliauskas D, Könst ZA, Pierens GK, Mándi A, Andrews KT, Skinner-Adams TS, Clarke ME, Narbutas PT, Sim DC, Cheney KL, Kurtán T, Garson MJ, Vanderwal CD: Catalyst-Controlled Stereoselective Synthesis Secures the Structure of the Antimalarial Isocyanoterpene Pustulosaisonitrile-1. J Org Chem; 2017 Dec 15;82(24):13313-13323

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Catalyst-Controlled Stereoselective Synthesis Secures the Structure of the Antimalarial Isocyanoterpene Pustulosaisonitrile-1.
  • Three new isocyanoditerpenes (5-7) have been characterized from Australian specimens of the nudibranch Phyllidiella pustulosa.
  • The planar structure and (3R,6S,7R) absolute configuration of pustulosaisonitrile-1 were deduced by spectroscopic analyses at 900 MHz informed by molecular modeling, DFT calculations, and computational NMR chemical shift predictions and by comparison of experimental electronic circular dichroism (ECD) data with TDDFT-ECD calculations for the truncated model compound 8.
  • A catalyst-controlled enantio- and diastereoselective total synthesis of the two most likely diastereomeric candidates for the structure of 5 solidified its (3R,6S,7R,10S,11R,14R) absolute configuration.
  • Three individual enantioselective methods provided stereochemical control at key positions, permitting an unambiguous final structural assignment.
  • Isocyanide 5 and synthetic diastereomers 5a and 5c showed activity against Plasmodium falciparum malaria parasites (IC<sub>50</sub> ∼1 μM).

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  • (PMID = 29124922.001).
  • [ISSN] 1520-6904
  • [Journal-full-title] The Journal of organic chemistry
  • [ISO-abbreviation] J. Org. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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4. Rodríguez V, Rivoira M, Guizzardi S, Tolosa de Talamoni N: Naringin prevents the inhibition of intestinal Ca&lt;sup&gt;2+&lt;/sup&gt; absorption induced by a fructose rich diet. Arch Biochem Biophys; 2017 Dec 15;636:1-10
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Naringin prevents the inhibition of intestinal Ca<sup>2+</sup> absorption induced by a fructose rich diet.
  • This study tries to elucidate the mechanisms by which fructose rich diets (FRD) inhibit the rat intestinal Ca<sup>2+</sup> absorption, and determine if any or all underlying alterations are prevented by naringin (NAR).
  • Male rats were divided into:.
  • 1) controls, 2) treated with FRD, 3) treated with FRD and NAR.
  • The intestinal Ca<sup>2+</sup> absorption and proteins of the transcellular and paracellular Ca<sup>2+</sup> pathways were measured.
  • Oxidative/nitrosative stress and inflammation parameters were evaluated.
  • FRD rats showed inhibition of the intestinal Ca<sup>2+</sup> absorption and decrease in the protein expression of molecules of both Ca<sup>2+</sup> pathways, which were blocked by NAR.
  • FRD rats showed an increase in the superoxide anion, a decrease in the glutathione and in the enzymatic activities of the antioxidant system, as well as an increase in the NO content and in the nitrotyrosine content of proteins.
  • They also exhibited an increase in both IL-6 and nuclear NF-κB.
  • All these changes were prevented by NAR.
  • In conclusion, FRD inhibit both pathways of the intestinal Ca<sup>2+</sup> absorption due to the oxidative/nitrosative stress and inflammation.
  • Since NAR prevents the oxidative/nitrosative stress and inflammation, it might be a drug to avoid alteration in the intestinal Ca<sup>2+</sup> absorption caused by FRD.
  • [MeSH-major] Calcium / metabolism. Calcium Signaling / drug effects. Dietary Carbohydrates / adverse effects. Flavanones / pharmacology. Fructose / adverse effects. Intestinal Absorption / drug effects
  • [MeSH-minor] Animals. Interleukin-6 / metabolism. Male. NF-kappa B / metabolism. Nitric Oxide / metabolism. Rats. Rats, Wistar

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 29122589.001).
  • [ISSN] 1096-0384
  • [Journal-full-title] Archives of biochemistry and biophysics
  • [ISO-abbreviation] Arch. Biochem. Biophys.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Dietary Carbohydrates; 0 / Flavanones; 0 / Interleukin-6; 0 / NF-kappa B; 30237-26-4 / Fructose; 31C4KY9ESH / Nitric Oxide; N7TD9J649B / naringin; SY7Q814VUP / Calcium
  • [Keywords] NOTNLM ; Fructose rich diet / Inflammation / Intestinal Ca(2+) absorption / Naringin / Nitrosative stress / Oxidative stress
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5. Zhou XD, Zhang C, He S, Zheng B, Zeng KW, Zhao MB, Jiang Y, Tu PF: New terpenoids and thiophene derivatives from the aerial parts of Artemisia sieversiana. Bioorg Med Chem Lett; 2017 Dec 15;27(24):5441-5445

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] New terpenoids and thiophene derivatives from the aerial parts of Artemisia sieversiana.
  • One new highly oxygenated nortriterpene, named sieverlactone (1), one new sesquiterpene, 1β,10β-epoxy-8α-acetoxyachillin (2), one new natural product, 5-propinyl-thiophene-2-carboxylic acid (3), and one new thiophene, 3-hydroxy-5-propinyl-2-acetyl-thiophene (4), together with 10 other known compounds (5-14), were isolated from the dried aerial parts of Artemisia sieversiana.
  • Their structures were elucidated by a combination of extensive spectroscopic analysis, including 1D, 2D NMR spectroscopic and mass spectrometric data.
  • Meanwhile, the stereochemistry of 1 and 2 was confirmed by single-crystal X-ray diffraction technique using Cu radiation.
  • All the isolates were evaluated for their anti-neuroinflammatory effects on the lipopolysaccharide-induced nitric oxide production in BV-2 murine microglial cells.
  • Compounds 2, 5, and 6 exhibited the significant activities with IC<sub>50</sub> values of 6.5 ± 0.5, 11.9 ± 0.7, and 10.1 ± 0.3 μM, respectively, comparable to the positive control, quercetin, with an IC<sub>50</sub> value of 16.3 ± 0.4 μM.

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  • [Copyright] Copyright © 2017 Elsevier Ltd. All rights reserved.
  • (PMID = 29122483.001).
  • [ISSN] 1464-3405
  • [Journal-full-title] Bioorganic & medicinal chemistry letters
  • [ISO-abbreviation] Bioorg. Med. Chem. Lett.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; Artemisia sieversiana / Nortriterpene / Sesquiterpene / Thiophene / X-ray diffraction
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6. Tallima H, Abou El Dahab M, Kareem S, Dalton JP, El Ridi R: Protection against Schistosoma haematobium infection in hamsters by immunization with Schistosoma mansoni gut-derived cysteine peptidases, SmCB1 and SmCL3. Vaccine; 2017 Dec 15;35(50):6977-6983

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Protection against Schistosoma haematobium infection in hamsters by immunization with Schistosoma mansoni gut-derived cysteine peptidases, SmCB1 and SmCL3.
  • We examined the immunogenicity and protective potential of SmCB1 and SmCL3 cysteine peptidases, alone and in combination, in hamsters challenged with S. haematobium.
  • For each of two independent experiments, eight Syrian hamsters were immunized twice with a three week-interval with 0 (controls), 20 µg SmCB1, 20 µg SmCL3, or 10 µg SmCB1 plus 10 µg SmCL3, and then percutaneously exposed eight weeks later to 100 S. haematobium cercariae.
  • Hamsters from each group were assessed for humoral and whole blood culture cytokine responses on day 10 post challenge infection, and examined for parasitological parameters 12 weeks post infection.
  • At day 10 post-infection we found that SmCB1 and SmCL3 elicited low antibody titres and weak but polarized cytokine type 2 responses.
  • Nevertheless, both cysteine peptidases, alone or in combination, evoked reproducible and highly significant reduction in challenge worm burden (>70%, P < 0.02) as well as a significant reduction in worm egg counts and viability.
  • The data support our previous findings and show that S. mansoni cysteine peptidases SmCB1 and SmCL3 are efficacious adjuvant-free vaccines that induce protection in mice and hamsters against both S. mansoni and S. haematobium.

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  • [Copyright] Copyright © 2017 Elsevier Ltd. All rights reserved.
  • (PMID = 29122387.001).
  • [ISSN] 1873-2518
  • [Journal-full-title] Vaccine
  • [ISO-abbreviation] Vaccine
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Cysteine peptidases / Hamsters / Oogram / Schistosoma haematobium / Schistosomiasis / Type 2 immune responses / Vaccine
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7. Ladwig KH, Fang X, Wolf K, Hoschar S, Albarqouni L, Ronel J, Meinertz T, Spieler D, Laugwitz KL, Schunkert H: Comparison of Delay Times Between Symptom Onset of an Acute ST-elevation Myocardial Infarction and Hospital Arrival in Men and Women &lt;65 Years Versus ≥65 Years of Age.: Findings From the Multicenter Munich Examination of Delay in Patients Experiencing Acute Myocardial Infarction (MEDEA) Study. Am J Cardiol; 2017 Dec 15;120(12):2128-2134

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Comparison of Delay Times Between Symptom Onset of an Acute ST-elevation Myocardial Infarction and Hospital Arrival in Men and Women <65 Years Versus ≥65 Years of Age.: Findings From the Multicenter Munich Examination of Delay in Patients Experiencing Acute Myocardial Infarction (MEDEA) Study.
  • Early administration of reperfusion therapy in acute ST-elevation myocardial infarctions (STEMI) is crucial to reduce mortality.
  • Although female sex and old age are key factors contributing to an inadequate long prehospital delay time, little is known whether women ≥65 years are a particular risk population.
  • Hence, we studied the interaction of sex and age (<65 years or ≥65 years) and the contribution of chest pain to delay time during STEMI.
  • Bedside interview data were collected in 619 STEMI patients from the Munich Examination of Delay in Patients Experiencing Acute Myocardial Infarction (MEDEA) study.
  • Sex and age group stratification disclosed an excess delay risk for women ≥65 years, accounting for a 2.39 (95% confidence interval (CI) 1.39 to 4.10)-fold higher odds to delay longer than 2 hours compared with all other patient groups including younger women (p ≤0.002).
  • Median delay time was 266 minutes in women ≥65 years and 148 minutes in younger women (p <0.001).
  • Chest pain during STEMI had the lowest frequency both in women (81%) and men ≥65 years (83%) and the highest frequency (95%) in younger women.
  • Experiencing non-chest pain was 2.32-fold (95% CI, 1.20 to 4.46, p <0.05) higher in women ≥65 years than in all other patients.
  • Mediation analysis disclosed that the effect accounted for only 9% of the variance.
  • Age specific educational strategies targeting women ≥65 years at risk are urgently needed.
  • To tailor adequate strategies, more research is required to understand age- and sex driven barriers to timely identification of ischemic symptoms.
  • [MeSH-major] Delayed Diagnosis. Electrocardiography. Hospitalization. Myocardial Revascularization. ST Elevation Myocardial Infarction / diagnosis. Thrombolytic Therapy. Time-to-Treatment / trends
  • [MeSH-minor] Aged. Cross-Sectional Studies. Female. Follow-Up Studies. Humans. Male. Middle Aged. Retrospective Studies

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 29122276.001).
  • [ISSN] 1879-1913
  • [Journal-full-title] The American journal of cardiology
  • [ISO-abbreviation] Am. J. Cardiol.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article; Multicenter Study
  • [Publication-country] United States
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8. Xianpei W, Sha W, Chuanyu G, Juanjuan Y, Chong C, Yongen S, Yu F, Zhenhao L: Tpeak-Tend dispersion as a predictor for malignant arrhythmia events in patients with vasospastic angina. Int J Cardiol; 2017 Dec 15;249:61-65

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Tpeak-Tend dispersion as a predictor for malignant arrhythmia events in patients with vasospastic angina.
  • BACKGROUND: Tpeak-Tend interval (Tp-e interval) in electrocardiogram (ECG) has been reported to predict malignant arrhythmia events (MAE) in ST-segment elevation myocardial infarction and ion channelopathy.
  • Tp-e interval and other ECG parameters as predictors for MAE was evaluated in patients with vasospastic angina (VA).
  • METHODS AND RESULTS: Sixty-two patients with VA (Non-MAE group) and 20 patients with VA complicated by MAE (MAE group) were enrolled in our Division of Cardiology between January 2010 and December 2015.
  • Continuous variables were analyzed by t-test and categorical variables by Chi-square analysis.
  • Patients with MAE showed greater QTc (corrected QT interval) dispersion (P=0.005), Tp-ec (corrected Tp-e) interval (P=0.001), Tp-ec dispersion (P<0.001) and Tp-e/QT ratio (P<0.001) than those in non-MAE groups when ST-segment elevated.
  • After elevated ST-segment returned, there were no significant differences in these ECG parameters between two groups (All P>0.05).
  • At univariate binary logistic regression analysis QTc dispersion (odds ratio(OR)=1.133; P=0.013), Tp-ec (OR=1.058; P=0.003), Tp-e/QT (OR=1.403; P=0.001), and Tp-ec dispersion (OR=1.497; P=0.004) were significantly associated with MAE.
  • At multivariable logistic regression analysis, Tp-ec dispersion remained a predictor of MAE.
  • Receiver operating characteristic (ROC) curve analysis showed that only AUC (Area under curve) of Tp-ec dispersion had significant difference with those in QTc dispersion (P<0.001), Tp-ec (P=0.003), and Tp-e/QT ratio (P=0.012), respectively.
  • CONCLUSIONS: QTc dispersion, Tp-ec, Tp-e/QT and Tp-ec dispersion were significantly increased in VA patients with MAE than those without MAE when coronary spasm was onset.
  • Prolonged Tp-ec dispersion was the best discriminators and a strong independent predictor of MAE in VA patients.

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  • [Copyright] Copyright © 2017. Published by Elsevier B.V.
  • (PMID = 29121758.001).
  • [ISSN] 1874-1754
  • [Journal-full-title] International journal of cardiology
  • [ISO-abbreviation] Int. J. Cardiol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Malignant arrhythmia events / Tp-e dispersion / Tp-e interval / Vasospastic angina
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9. Kim Y, Cho JS, Cho WK, Yoon HE, Hong YA, Chang YK, Yang CW, Kim SY, Hwang HS: Retinopathy and left ventricular hypertrophy in patients with chronic kidney disease: Interrelationship and impact on clinical outcomes. Int J Cardiol; 2017 Dec 15;249:372-376

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Retinopathy and left ventricular hypertrophy in patients with chronic kidney disease: Interrelationship and impact on clinical outcomes.
  • BACKGROUND: Retinopathy and left ventricular hypertrophy (LVH) are representative markers of microvascular and cardiac dysfunction in patients with chronic kidney disease (CKD).
  • However, their relationship and their combined effects on clinical outcomes are unknown.
  • METHODS: We included 401 patients with nondialysis-dependent CKD stage 3-5 who had been examined with fundus photography for diabetic or hypertensive retinopathy.
  • The presence of LVH was identified by echocardiography.
  • The clinical significance of retinopathy and LVH was evaluated in terms of the rate of renal function decline and for any cardiovascular event (CVE)/death.
  • RESULTS: CKD patients with retinopathy had a higher prevalence of LVH than those without retinopathy (38.9% vs. 27.6%, P=0.017).
  • The presence of retinopathy was independently associated with LVH (odds ratio 1.69, 95% confidence interval [CI] 1.02, 2.80).
  • Compared with subjects without either retinopathy or LVH, the coexistence of retinopathy and LVH was independently associated with rapid renal function decline (β=-3.28; 95% CI -6.52, -0.04), whereas retinopathy or LVH alone were not.
  • Patients with both retinopathy and LVH had a higher risk of CVE/death (adjusted hazard ratio 2.75; 95% CI 1.44, 5.26) than patients with either factor alone.
  • A significant synergistic interaction was observed between retinopathy and LVH to predict CVE/death (P for interaction=0.049).
  • CONCLUSIONS: Retinopathy was independently associated with LVH.
  • The coexistence of retinopathy and LVH was associated with higher risks of CKD progression and CVE/death than was either factor alone, and their combined effects synergized to predict the risk of CVE/death.

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  • [Copyright] Copyright © 2017 Elsevier Ireland Ltd. All rights reserved.
  • (PMID = 29121742.001).
  • [ISSN] 1874-1754
  • [Journal-full-title] International journal of cardiology
  • [ISO-abbreviation] Int. J. Cardiol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Cardiovascular event / Chronic kidney disease / Left ventricular hypertrophy / Retinopathy
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10. Zachariah D, Stevens D, Sidorowicz G, Spooner C, Rowell N, Taylor J, Kay R, Salek MS, Kalra PR, LIVE:LIFE study investigators: Quality of life improvement in older patients with heart failure initiated on ivabradine: Results from the UK multi-centre LIVE:LIFE prospective cohort study. Int J Cardiol; 2017 Dec 15;249:313-318

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Quality of life improvement in older patients with heart failure initiated on ivabradine: Results from the UK multi-centre LIVE:LIFE prospective cohort study.
  • AIMS: LIVE:LIFE is a multi-centre, open-label, prospective observational cohort study assessing health-related quality of life (HRQoL) in older patients with chronic heart failure (CHF) following initiation of ivabradine.
  • The primary endpoint is change in Minnesota Living with Heart Failure Questionnaire (MLWHFQ) total score after 6months.
  • METHODS AND RESULTS: Consenting patients aged ≥70years with CHF, in whom ivabradine was initiated within its licensed indication, were enrolled.
  • Demographic, clinical and HRQoL (MLWHFQ, SF-12) data were collected at baseline (V1), 2 (V2) and 6months (V3).
  • Over 14months, 240 patients were recruited from 44 UK centres.
  • Ninety-nine (41%) were female and 28% aged ≥80years.
  • Aetiology was ischaemic in 152 (63%) and 59% had been diagnosed with CHF for ≤2yrs.
  • 52% of patients were New York Heart Association (NYHA) Class III and 57% had left ventricular ejection fraction <35%.
  • 57% received beta-blockers.
  • Patients had multiple comorbidities (144 (60%) hypertension, 105 (44%) asthma/COPD, 80 (33%) diabetes) and were prescribed a mean of 9±3 daily medications.
  • Resting heart rate was 83bpm at baseline and fell 13bpm by V3.
  • In patients completing both visits (n=187), comparing V3 to baseline: MLWHFQ total score improved by 9 points (p<0.0001, 95% CI: 7-12); 30% of patients improved ≥1 NYHA class and global assessment improved from patient (59%) and physician (60%) perspectives.
  • 88% of patients completing V3 were still taking ivabradine.
  • CONCLUSIONS: These contemporary prospective UK data demonstrate improvements in HRQoL and functional status with ivabradine therapy in typical older CHF patients.
  • Despite comorbidities and polypharmacy, ivabradine was well tolerated.

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 29121732.001).
  • [ISSN] 1874-1754
  • [Journal-full-title] International journal of cardiology
  • [ISO-abbreviation] Int. J. Cardiol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Elderly / HRQoL / Health-related quality of life / Heart failure / Ivabradine / MLWHFQ
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