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About ADEMPAS
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About ADEMPAS®▼ (riociguat)

Updated on 20/02/2019

CARDIOVASCULAR

ADEMPAS is a member of a class of therapeutic agents called soluble guanylate cyclase stimulators (sGC stimulators), and is used for the treatment of Pulmonary Arterial Hypertension (PAH) and Chronic Thromboembolic Pulmonary Hypertension (CTEPH).

In PAH, ADEMPAS is licenced as monotherapy or in combination with endothelin receptor antagonists (ERA’s), for the treatment of adult patients with PAH with WHO Functional Class (FC) II to III to improve exercise capacity.

In CTEPH, ADEMPAS is licenced for the treatment of adult patients with WHO functional class II to III with:

  • inoperable CTEPH,
  • persistent or recurrent CTEPH after surgical treatment, to improve exercise capacity.

Mode of action

ADEMPAS: a PH treatment with a dual mode of action1

NO - nitric oxide; sGC - soluble guanylate cyclase; cGMP - cyclic guanosine monophosphate; GTP - guanosine triphosphate

  • Normally, NO binds to and stimulates sGC2
  • In many PH patients NO is depleted due to endothelial dysfunction3
  • NO deficiency results in sGC being understimulated3
  • sGC facilitates cGMP synthesis1
  • ADEMPAS stimulates sGC independently of NO1
  • ADEMPAS also sensitises sGC to endogenous NO by stabilising the NO-sGC binding3

ADEMPAS is a sGC stimulator, an enzyme in the cardiopulmonary system and the receptor for Nitric Oxide (NO).

When NO binds to sGC, the enzyme catalyses synthesis of the signalling molecule cGMP. Intracellular cGMP has an important part in regulating processes that influence vascular tone, proliferation, fibrosis and inflammation. PH is associated with endothelial dysfunction, impaired synthesis of NO, and insufficient stimulation of the NO-sGC-cGMP pathway.

ADEMPAS has a dual mode of action. It sensitises sGC to endogenous NO by stabilising the NO-sGC binding. ADEMPAS also directly stimulates sGC independently of NO. ADEMPAS restores the NO-sGC-cGMP pathway and leads to increased generation of cGMP.

ADEMPAS restores the NO-sGC-cGMP pathway resulting in an improvement of pulmonary vascular hemodynamics and an increase in exercise ability.

ADEMPAS is currently reimbursed by NHS England for CTEPH patients in FC II and III, and for PAH patients in FC III.

References

  1. O’Callaghan DS, Savale L, Montani D, et al. Treatment of pulmonary arterial hypertension with targeted therapies. Nature Rev Drug Cardiol. 2011;8:526–538.
  2. Stasch J-P, Pacher P, Evgenov OV, et al. Soluble guanylate cyclase as an emerging therapeutic target in cardiopulmonary disease. Circulation. 2011;123:2263–2273.
  3. ADEMPAS Summary of Product Characteristics.

Supporting documentation

Prescribing Information | Summary of Product Characteristics | Patient Information Leaflet

GB-ADE-00074 | Date of Preparation: February 2019