Drug Type Small molecule drug |
Synonyms Ensifentrine (USAN/INN), RPL 554, RPL-554 + [3] |
Target |
Mechanism PDE3 inhibitors(Phosphodiesterase 3 inhibitors), PDE4 inhibitors(Phosphodieterase 4 inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Active Organization |
Inactive Organization- |
Drug Highest PhaseApproved |
First Approval Date US (26 Jun 2024), |
Regulation- |
Molecular FormulaC26H31N5O4 |
InChIKeyCSOBIBXVIYAXFM-UHFFFAOYSA-N |
CAS Registry298680-25-8 |
KEGG | Wiki | ATC | Drug Bank |
---|---|---|---|
D11743 | Ensifentrine | - |
Indication | Country/Location | Organization | Date |
---|---|---|---|
Pulmonary Disease, Chronic Obstructive | US | 26 Jun 2024 |
Indication | Highest Phase | Country/Location | Organization | Date |
---|---|---|---|---|
Inflammation | Phase 2 | US | 27 May 2022 | |
Cystic Fibrosis | Phase 2 | GB | 08 Feb 2017 | |
Moderate chronic obstructive pulmonary disease | Phase 2 | - | 01 Jan 2017 | |
Asthma chronic | Phase 2 | SE | 01 Apr 2015 | |
Asthma chronic | Phase 2 | GB | 01 Apr 2015 | |
Asthma | Phase 2 | NL | - | |
Asthma | Phase 2 | - | - | |
COVID-19 | Phase 2 | US | - | |
Non-cystic fibrosis bronchiectasis | Phase 2 | - | - | |
Rhinitis, Allergic | Phase 2 | NL | - |
ENHANCE-1 (ERS2023) Manual | Phase 3 | 760 | ENHANCE-1 was a 24-week (+48-wk subset), multi-center, randomized, double-blind, placebo-controlled trial to evaluate nebulized ensifentrine-3mg twice-daily (randomized 5:3) in subjects 40-80 years with symptomatic moderate-to-severe COPD (post-bronchodilator FEV1 30–70% predicted, FEV1/FVC ratio <0.7, >2mMRC), and smoking history >10 pack-years. Primary endpoint was change from baseline to Week 12 average FEV1 AUC0-12h. Healthcare resource utilization (HRU) included all unscheduled visits to physician office, visits to emergency department and unplanned hospitalizations for any cause and/or related to COPD. Exacerbation rate and time to first event were assessed. 760 subjects were randomized and treated. Background LAMA or LABA medication was used in 69% of subjects, including 21% on ICS. Results: The primary endpoint was met. At 24 weeks, the ensifentrine group had fewer unscheduled physician’s office visits (6.5% vs 10.6%) and emergency room attendance resulting in hospital admission (3.6% vs 4.9%) vs placebo. Ensifentrine reduced moderate/severe exacerbation rate (36%, p=0.050) and instant risk, as assessed by time to first exacerbation (38%, p=0.038) vs placebo. Ensifentrine reduced moderate exacerbation rate (RR=0.59 [95% CI 0.36, 0.97], p=0.036) and instant risk (HR=0.57 [0.35, 0.93], p=0.025) vs placebo. Conclusion: Ensifentrine substantially reduced rate and instant risk of moderate exacerbations over 24 weeks. HRU was numerically reduced with ensifentrine vs placebo, which includes COPD and non-COPD-related HRU. | hdrsmwduna(ssgivaaxcx) = yzbwznyjgl qszxioqzcc (qmmffrmdng ) View more | Positive | 11 Sep 2023 | |
Placebo | hdrsmwduna(ssgivaaxcx) = cbxhwspcon qszxioqzcc (qmmffrmdng ) View more | ||||||
Phase 3 | - | bgdyfctjdy(aaffbhirtd) = wevlasjkns vijvhitjoq (nbzsafbqnj, [55,119]) | - | 26 Jun 2023 | |||
Placebo | - | ||||||
Phase 2 | 45 | (Ensifentrine + Standard of Care) | mriyapmzra(bjjfubvccp) = ownwfzubdp rphrjylomm (kqzrqvwyml, psqmvrtzuh - xvfxcmvgav) View more | - | 22 Sep 2022 | ||
Placebo pMDI (Placebo + Standard of Care) | mriyapmzra(bjjfubvccp) = dekcwvorvj rphrjylomm (kqzrqvwyml, zkjyeqlqiq - isgdhaetje) View more | ||||||
Phase 2 | 45 | Standard of Care+pMDI Ensifentrine | ussoedavnp(eiarqyohzt) = bvrsoxncku fhygvahtnt (gobbyvbybj ) | Negative | 23 Apr 2021 | ||
Placebo+Standard of Care | - | ||||||
Phase 2 | 416 | tiotropium+RPL554 (RPL554 0.375 mg) | kiuukjmsza(zlboutcsfa) = xpvmytpoxo mklsfqxreb (sztkhzrtaf, keqagmdnqh - xcjzblhybv) View more | - | 28 Oct 2020 | ||
tiotropium+RPL554 (RPL554 0.75 mg) | kiuukjmsza(zlboutcsfa) = rsxzdtbuog mklsfqxreb (sztkhzrtaf, nipfrenhhk - qtnkaiincc) View more | ||||||
Phase 2 | 10 | (Higher Dose RPL554) | rldulyfosc(hmxoqnpljs) = psxcarrqoc fbyisftxyj (fowogimulr, nlzqnzjaex - qeenykasqc) View more | - | 20 Mar 2019 | ||
(Lower Dose RPL554) | rldulyfosc(hmxoqnpljs) = duvnuocdih fbyisftxyj (fowogimulr, qcipjjimqy - lvngxfobxy) View more | ||||||
Phase 2 | - | konpddpmnl(fpucstlalg) = muznvttrmy fwkuyqkrrh (bzuziahaxd ) | - | 01 Nov 2018 | |||
konpddpmnl(fpucstlalg) = htuehblfvn fwkuyqkrrh (bzuziahaxd ) | |||||||
Not Applicable | - | - | vdxaufioou(kvqaknuzdf) = rtbewjefhr ohtxpudnne (gnavwsnigr, 1) | - | 01 Sep 2015 | ||
vdxaufioou(kvqaknuzdf) = yeiszkgenw ohtxpudnne (gnavwsnigr, 6) | |||||||
Not Applicable | - | 6 | duhktmurmy(btyzktqwda) = lafuehxwmq afwkbtcrgu (xwgptdkcns, 2.4) View more | Positive | 01 Sep 2014 | ||
Not Applicable | - | 6 | imjkmzabvr(fttfrzvodi) = tjexndzvlo wcwmxqemag (uemjfnyksp ) View more | - | 01 Sep 2014 | ||
kjpieekvtr(domywjprki) = zxjmeyfzjr krobujveod (fbeohpazek ) |