PMID- 26011143
OWN - NLM
STAT- MEDLINE
DCOM- 20151221
LR  - 20171116
IS  - 1875-9114 (Electronic)
IS  - 0277-0008 (Linking)
VI  - 35
IP  - 5
DP  - 2015 May
TI  - Riociguat: a novel new drug for treatment of pulmonary hypertension.
PG  - 502-19
LID - 10.1002/phar.1592 [doi]
AB  - Riociguat is the first approved medication from the novel class of soluble 
      guanylate cyclase (sGC) stimulators and the only agent approved for treating both 
      chronic thromboembolic hypertension (CTEPH) and pulmonary arterial hypertension 
      (PAH). The novel mechanism of riociguat lies in its ability to restore the 
      homeostatic and therapeutic effects of nitric oxide that are diminished as a 
      result of phenotypic alterations associated with pulmonary hypertension (PH). 
      Improvements in 6-minute walk distance (6MWD) in patients with PAH during the 
      phase 3 PATENT-1 trial were comparable to other oral agents approved for the 
      treatment of PAH. Improvements in 6MWD in patients with CTEPH during the phase 3 
      CHEST-1 trial were greater than those previously observed with other oral 
      PAH-directed therapies. Hypotension is the dose-limiting adverse effect of 
      riociguat and dose titration is performed gradually according to systolic blood 
      pressure. Riociguat was tolerated at maximal doses by most patients during 
      PATENT-1 and CHEST-1 and was well tolerated during long-term extension studies. 
      Key factors to consider with riociguat are a patient's systolic blood pressure, 
      drug interactions mediated by CYP1A1, CYP3A4, and P-glycoprotein, cost, and 
      teratogenicity requiring enrollment in a Risk Evaluation and Mitigation Strategy 
      program. Recently published guidelines recommend riociguat monotherapy as an 
      option for treatment-naive patients with World Health Organization Functional 
      Class (WHO FC) II or III symptoms or as add-on therapy for patients with 
      persistent WHO FC III or IV symptoms being treated with an ERA or inhaled 
      prostanoid. Postmarketing experience and ongoing clinical investigations will 
      further define the safety and role of riociguat in patients with PAH and other 
      types of PH.
CI  - (c) 2015 Pharmacotherapy Publications, Inc.
FAU - Makowski, Charles T
AU  - Makowski CT
AD  - Department of Pharmacy Services, Henry Ford Hospital, Detroit, Michigan.
FAU - Rissmiller, Richard W
AU  - Rissmiller RW
AD  - Division of Pulmonary and Critical Care, Medical University of South Carolina, 
      Charleston, South Carolina.
FAU - Bullington, Wendy M
AU  - Bullington WM
AD  - Department of Pharmacy Services, Medical University of South Carolina, 
      Charleston, South Carolina.
LA  - eng
PT  - Journal Article
PT  - Review
PL  - United States
TA  - Pharmacotherapy
JT  - Pharmacotherapy
JID - 8111305
RN  - 0 (Pyrazoles)
RN  - 0 (Pyrimidines)
RN  - 0 (Receptors, Cytoplasmic and Nuclear)
RN  - EC 4.6.1.2 (Guanylate Cyclase)
RN  - EC 4.6.1.2 (Soluble Guanylyl Cyclase)
RN  - RU3FE2Y4XI (riociguat)
SB  - IM
MH  - Clinical Trials, Phase III as Topic
MH  - Guanylate Cyclase/*metabolism
MH  - Humans
MH  - Hypertension, Pulmonary/*drug therapy/etiology
MH  - Pyrazoles/pharmacokinetics/pharmacology/*therapeutic use
MH  - Pyrimidines/pharmacokinetics/pharmacology/*therapeutic use
MH  - Receptors, Cytoplasmic and Nuclear/*metabolism
MH  - Soluble Guanylyl Cyclase
OTO - NOTNLM
OT  - pulmonary hypertension
OT  - riociguat
OT  - soluble guanylate cyclase
EDAT- 2015/05/27 06:00
MHDA- 2015/12/22 06:00
CRDT- 2015/05/27 06:00
PHST- 2015/05/27 06:00 [entrez]
PHST- 2015/05/27 06:00 [pubmed]
PHST- 2015/12/22 06:00 [medline]
AID - 10.1002/phar.1592 [doi]
PST - ppublish
SO  - Pharmacotherapy. 2015 May;35(5):502-19. doi: 10.1002/phar.1592.