DSP-2230 / Sumitomo Pharma, AlphaNavi - LARVOL DELTA

A novel Nav1.7, Nav1.8, and Nav1.9 blocker, ANP-230, has broad analgesic efficacy in preclinical pain models with favorable safety margins. (PubMed, Biochem Biophys Res Commun) - "Furthermore, when concurrently administered with pregabalin and morphine, ANP-230 potentiated their anti-allodynic effects. Hence, ANP-230 has potential as a broad-spectrum analgesic with a favorable safety profile. Our study sheds light on a strategy utilizing a peripherally restricted compound that preferentially inhibits Nav1.7, Nav1.8, and Nav1.9 in chronic pain conditions."

Journal • Preclinical • Neuralgia • Pain • NAV1

Unique electrophysiological property of a novel Nav1.7, Nav1.8, and Nav1.9 sodium channel blocker, ANP-230. (PubMed, Biochem Biophys Res Commun) - "Finally, ANP-230 reduced excitability of rat dorsal root ganglion neurons in a concentration dependent manner. Collectively, these promising results indicate that ANP-230 could be a potent drug for neuropathic pain."

Journal • Cardiovascular • Neuralgia • Pain • NAV1

Analgesic effects of a novel sodium channel blocker on a mouse model of episodic pain syndrome (Neuroscience 2023) - "Overall, our results clearly suggest that ANP-230 has an analgesic effect on FEPS and that this results from reduced DRG neuron hyperexcitability. It is highly likely that the effects of this non-opioid drug will be of clinical significance not only for FEPS but also for other peripheral nerve pain symptoms."

Preclinical • Addiction (Opioid and Alcohol) • CNS Disorders • Musculoskeletal Pain • Neuralgia • Pain

Reduced pain sensitivity of episodic pain syndrome model mice carrying a Nav1.9 mutation by ANP-230, a novel sodium channel blocker. (PubMed, Heliyon) - "Furthermore, ANP-230 suppressed the repetitive firing of dorsal root ganglion neurons of these mutant mice. Our results clearly demonstrate that ANP-230 is an effective analgesic for familial episodic pain syndrome resulting from DRG neuron hyperexcitability, and that such analgesic effects are likely to be of clinical significance."

Journal • Preclinical • Addiction (Opioid and Alcohol) • Immunology • Musculoskeletal Pain • Pain

Cardiac biomarkers as indicators of right ventricular dysfunction and recovery in chronic thromboembolic pulmonary hypertension patients after balloon pulmonary angioplasty therapy - a cardiac magnetic resonance imaging cohort study. (PubMed, Pulm Circ) - "Biomarker level cut-offs [NT-proBNP 347 ng/L (area under the curve (AUC) 0.91), MR-proANP 230 pg/L (AUC 0.78), PAPP-A 14.5 mU/L (AUC 0.81), and sST2 48.0 ng/ml (AUC 0.88)] indicated a RVEF ≤ 35% at baseline...In chronic thromboembolic pulmonary hypertension patients, cardiac magnetic resonance imaging findings illustrate right heart failure and recovery after balloon pulmonary angioplasty therapy. Cardiac biomarker levels correlate with right heart parameters at baseline and their dynamics after therapy."

Biomarker • Clinical • Journal • Cardiovascular • Congestive Heart Failure • Heart Failure • Hypertension • Pulmonary Arterial Hypertension • Pulmonary Disease • Pulmonary Embolism • Respiratory Diseases • MRI

SAFETY AND PHARMACOKINETICS PROFILES OF DSP-2230, A NOVEL SODIUM CHANNEL BLOCKER (NeuPSIG 2017) - "These findings suggest that DSP-2230 has positive potential as a drug for the treatment of neuropathic pain without CV or CNS side-effects, which are present with current drugs such as non-selective sodium channel blockers and anti-epileptics."

Biosimilar • Demo Pain • Epilepsy • Pain

Dainippon Sumitomo's establishment of a curve out-venture aiming for early commercialization in the pain area [Google translation] (Mix Online) - "Dainippon Sumitomo Pharma and Kyoto University Innovation Capital (Kyoto iCAP), affiliated with Kyoto University, established on March 28 a curve-out venture 'AlphaNavi Pharma (Kyoto City, Yoshihiro Oyamada),' promoting research and development in pain areas, announced, with a license to manufacture, develop and market DSP-2230, a company created by Dainippon Sumitomo Pharma in-house, the company hopes to start Phase 2 in the second half of fiscal 2019 for childhood pain and seizure disorder in children."

Commercial • Licensing / partnership • New P2 trial