Effects of riociguat: A Synthesis of Findings from 20 Studies

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Original Abstract of the Article

Major Research Findings

Riociguat is a promising drug for treating pulmonary hypertension, particularly in patients with chronic obstructive pulmonary disease (COPD), pulmonary arterial hypertension (PAH), and chronic thromboembolic pulmonary hypertension (CTEPH). 3 It has been shown to improve pulmonary hemodynamics by reducing pulmonary vascular resistance and easing the workload on the right ventricle. 3 Riociguat is well absorbed orally, with minimal food effects, and systemic exposure is proportional to the dose. 10 The drug has been demonstrated to be safe and effective in both short-term and long-term studies. 3

While riociguat is generally well-tolerated, there are some potential risks associated with its use. Renal impairment can lead to reduced clearance of riociguat, potentially increasing the risk of side effects. 9 Smoking can also influence the exposure to riociguat, further impacting the risk of side effects. 9

Benefits and Risks

Benefit Summary

Riociguat can improve symptoms of pulmonary hypertension, such as shortness of breath and fatigue. 3 It can also slow the progression of the disease and improve quality of life for patients.

Risk Summary

Riociguat may cause side effects such as headache, dizziness, nausea, and indigestion. 3 Patients with impaired kidney function and smokers should consult with their doctor before taking riociguat. 9

Comparison Between Studies

Commonalities Between Studies

Multiple studies agree that riociguat can effectively reduce pulmonary vascular resistance in patients with pulmonary hypertension. 3 7 Furthermore, research consistently demonstrates that riociguat is a generally safe medication. 3 10 9

Differences Between Studies

The effectiveness of riociguat can vary depending on the type of disease and the individual patient. 6 The frequency and severity of side effects can also vary between patients. 9

Consistency and Contradictions in the Findings

Multiple studies consistently show that riociguat can effectively reduce pulmonary vascular resistance in pulmonary hypertension patients. 3 7 However, its effectiveness can vary depending on the specific type of pulmonary hypertension and individual patient characteristics. 6 Further research is needed to refine our understanding of its effectiveness in different patient populations.

Considerations for Applying Research in Real-Life Settings

Riociguat is a medication that should be taken under the guidance of a doctor. 3 It is crucial for pregnant or breastfeeding women to consult with their doctor before taking riociguat. 3 Patients with kidney problems or smokers should also discuss riociguat use with their physician. 9

Limitations of Current Research

Research on riociguat is still ongoing, with some limitations. 3 Long-term safety and efficacy data require further investigation.

Future Research Directions

More research is needed to assess the long-term safety and effectiveness of riociguat. Studies investigating the optimal dosage and administration methods for different patient populations are also necessary. 10 Additionally, research should explore the combined effects of riociguat with other medications. 2

Conclusion

Riociguat shows potential as a treatment for pulmonary hypertension, particularly in patients with COPD, PAH, and CTEPH. 3 7 However, further research is required to better understand its long-term safety and effectiveness. If you are considering riociguat, it is essential to discuss it with your doctor. 3

Literature analysis of 20 papers
Positive Content
17
Neutral Content
0
Negative Content
3
Article Type
3
1
2
4
20
1.

Modulation of vascular contraction via soluble guanylate cyclase signaling in a novel ex vivo method using rat precision-cut liver slices.

Author: OldenburgerAnouk, BirkGerald, SchlepützMarco, BroermannAndre, StierstorferBirgit, PullenSteven S, RippmannJörg F

Drug screening
Vessel relaxation

Precision cut liver slices from normal and fibrotic rat livers were used to assess blood vessel function in non-alcoholic steatohepatitis. The study identified the role of the sGC pathway for vessel relaxation of fibrotic liver tissue, suggesting potential for drug screening and development.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

2.

Balloon pulmonary angioplasty versus riociguat in inoperable chronic thromboembolic pulmonary hypertension (MR BPA): an open-label, randomised controlled trial.

Author: KawakamiTakashi, MatsubaraHiromi, ShinkeToshiro, AbeKohtaro, KohsakaShun, HosokawaKazuya, TaniguchiYu, ShimokawaharaHiroto, YamadaYoshitake, KataokaMasaharu, OgawaAiko, MurataMitsushige, JinzakiMasahiro, HirataKenichi, TsutsuiHiroyuki, SatoYasunori, FukudaKeiichi

This study aims to compare the safety and effectiveness of balloon pulmonary angioplasty (BPA) and riociguat in treating patients with inoperable chronic thromboembolic pulmonary hypertension (CTEPH).

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

3.

Acute effects of riociguat in borderline or manifest pulmonary hypertension associated with chronic obstructive pulmonary disease.

Author: GhofraniHossein A, StaehlerGerd, GrünigEkkehard, HalankMichael, MitrovicVeselin, UngerSigrun, MueckWolfgang, FreyReiner, GrimmingerFriedrich, SchermulyRalph T, BehrJuergen

PH hemodynamics improvement

A single dose of riociguat significantly improved pulmonary hemodynamics in patients with COPD-associated PH without affecting lung function or gas exchange.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

5.

The 10th International Conference on cGMP 2022: recent trends in cGMP research and development-meeting report.

Author: FriebeAndreas, KraehlingJan R, RusswurmMichael, SandnerPeter, SchmidtkoAchim

Achondroplasia treatment
Bone formation disorder treatment
Chronic heart failure treatment
Coronary artery disease treatment
Dementia treatment
Erectile dysfunction treatment
Irritable bowel syndrome treatment
Neurodegenerative disease treatment
Pulmonary hypertension treatment
cGMP increase risk

cGMP-increasing therapies are used for various diseases, including erectile dysfunction, pulmonary hypertension, and chronic heart failure. This review summarizes the 10th cGMP Conference, highlighting recent advances in understanding cGMP signaling pathways and therapeutic implications.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

7.

Riociguat prevents hyperoxia-induced lung injury and pulmonary hypertension in neonatal rats without effects on long bone growth.

Author: DondaKeyur, ZambranoRonald, MoonYounghye, PercivalJustin, VaidyaRuben, Dapaah-SiakwanFredrick, LuoShihua, DuncanMatthew R, BaoYong, WangLuqing, QinLing, BennyMerline, YoungKaren, WuShu

BPD prevention
Long bone growth
PH prevention

Riociguat was found to be beneficial in preventing hyperoxia-induced lung injury and pulmonary hypertension (PH) in newborn rats without affecting long bone growth. This suggests that riociguat may be a potential novel agent for preventing bronchopulmonary dysplasia (BPD) and PH in neonates.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

Mechanism of thromboxane receptor-induced vasoconstriction in human saphenous vein.

Author: OzenGulsev, AljesriKhadija, CelikZeynep, TurkyılmazGulsum, TurkyılmazSaygın, TeskinOnder, NorelXavier, TopalGokce

SV graft failure prevention
Platelet aggregation
Vasoconstriction

Thromboxane A2 is involved in saphenous vein graft failure by inducing vasoconstriction and platelet aggregation.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

10.

Absorption of riociguat (BAY 63-2521): bioavailability, food effects, and dose proportionality.

Author: BeckerCorina, FreyReiner, HesseChristiane, UngerSigrun, ReberMichael, MückWolfgang

Treatment of pulmonary arterial hypertension

Riociguat, a soluble guanylate cyclase (sGC) stimulator, demonstrates complete oral absorption, no clinically relevant food effects, and dose-proportional systemic exposure, supporting its suitability for individualized dose adjustment.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

12.

Hemodynamic Effects of a Soluble Guanylate Cyclase Stimulator, Riociguat, and an Activator, Cinaciguat, During NO-Modulation in Healthy Pigs.

Author: NæsheimTorvind, HowOle-Jakob, MyrmelTruls

Cardiovascular disease treatment

This study characterized the integrated hemodynamic impact of the sGC stimulator riociguat and the activator cinaciguat in healthy juvenile pigs. Both drugs had a more pronounced vasodilatory effect in systemic circulation than pulmonary circulation. Riociguat acted additively with NO, while cinaciguat blocked the endogenous NO effect on vascular control.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

13.

Impact of Innovative Treatment Using Biological Drugs for the Modulation of Diffuse Cutaneous Systemic Sclerosis: A Systematic Review.

Author: Fernández-LázaroDiego, Iglesias-LázaroMaría, GarrosaEvelina, Rodríguez-GarcíaSaray, Jerves DonosoDavid, Gutiérrez-AbejónEduardo, Jorge-FinniganConrado

dcSSc treatment

This systematic review summarizes the current evidence on the effects of biological drugs on pulmonary function, skin disease, and health status in patients with diffuse cutaneous systemic sclerosis (dcSSc). While biological drugs like tocilizumab, belimumab, riociguat, abatacept, and romilkimab showed trends towards improvement, there was no significant benefit on health status compared to control groups. These drugs may offer a new therapeutic strategy for dcSSc, potentially promoting anti-fibrotic activity.

Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

15.

Medications for the treatment of pulmonary arterial hypertension: a systematic review and network meta-analysis.

Author: PitreTyler, SuJohnny, CuiSonya, ScanlanRyan, ChiangChristopher, HusnudinovRenata, KhalidMuhammad Faran, KhanNadia, LeungGareth, MikhailDavid, SaadatPakeezah, ShahidShaneela, MahJasmine, MielniczukLisa, ZeraatkarDena, MehtaSanjay

Improved walking distance
Reduced clinical worsening
Reduced mortality

Combination therapy with endothelin receptor antagonist (ERA) plus phosphodiesterase-5 inhibitors (PDE5i) is the most effective treatment for pulmonary arterial hypertension (PAH). This combination reduces clinical worsening, as do ERA or PDE5i alone and riociguat monotherapy. PDE5i, intravenous/subcutaneous prostanoids, and riociguat probably reduce mortality as compared to placebo. Combination therapy with ERA+PDE5i and riociguat probably increase 6-min walk distance as compared to placebo.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Meta-AnalysisA statistical technique that integrates the results of multiple studies to draw more general conclusions about a particular issue.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.
Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.

Language : English

16.

Effect of riociguat on right ventricular function in patients with pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension.

Author: BenzaRaymond L, GhofraniHossein-Ardeschir, GrünigEkkehard, HoeperMarius M, JansaPavel, JingZhi-Cheng, KimNick H, LanglebenDavid, SimonneauGérald, WangChen, BusseDennis, MeierChristian, GhioStefano

Pulmonary arterial hypertension treatment

This review examines the efficacy and safety of riociguat, a medication used to treat pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH), in clinical trials. The review found that riociguat is effective in treating PAH and CTEPH and that its effects are sustained over the long term.

Clinical Trial, Phase IIIA Phase III trial is a trial that further rigorously verifies the efficacy and safety of a new drug or treatment, whose efficacy and safety have been confirmed in a Phase II trial, in a large number of patients, and evaluates whether it is superior to existing treatments.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

17.

Inhaled nitric oxide to control platelet hyper-reactivity in patients with acute submassive pulmonary embolism.

Author: KlineJeffrey A, PuskarichMichael A, PikeJonathan W, ZagorskiJohn, AlvesNathan J

Reduced platelet hyperreactivity

The study evaluated the effects of inhaled nitric oxide (NO) on platelet hyper-reactivity in patients with submassive pulmonary embolism (PE). Despite successful NO delivery, no significant effects were observed on platelet oxygen consumption or agonist-stimulated parameters. However, pharmacological activation of soluble guanylate cyclase (sGC) significantly reduced platelet cytosolic calcium levels.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.

Language : English

20.

Mechanistic insights into cell-free hemoglobin-induced injury during septic shock.

Author: WangJeffrey, ApplefeldWillard N, SunJunfeng, SolomonSteve B, FengJing, CouseZoe G, RisoleoThomas F, DannerRobert L, TejeroJesús, LertoraJuan, AlipourElmira, BasuSwati, SachdevVandana, Kim-ShapiroDaniel B, GladwinMark T, KleinHarvey G, NatansonCharles

Cardiogenic shock
Multiorgan failure
Pulmonary hypertension

This study investigated whether elevated cell-free hemoglobin (CFH) levels contribute to sepsis-associated injuries in beagles. CFH significantly increased pulmonary arterial pressures and worsened shock and multiorgan failure in both septic and nonseptic animals. CFH administration also worsened oxygen exchange and lung injury in infected animals. These findings suggest that CFH may be a potential therapeutic target for sepsis.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

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