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Camizestrant-induced heart rate reduction is mediated via a sinoatrial node pacemaker channel mechanism - PubMed

5 hours ago
  • #Camizestrant
  • #Pacemaker Channel Mechanism
  • #Heart Rate Reduction
  • Camizestrant, a next-generation selective estrogen receptor degrader and antagonist, causes a reversible, dose- and time-dependent reduction in heart rate in clinical and nonclinical studies.
  • In dogs and rats, camizestrant administration led to significant heart rate reductions, which persisted even after blocking sympathetic and parasympathetic nervous system inputs, indicating a direct cardiac effect.
  • The mechanism involves inhibition of the hyperpolarization-activated cyclic nucleotide-gated channel 4 (HCN4) and the 'funny' pacemaker current (If) in sinoatrial node cells, reducing pacemaker activity and heart rate.