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LT1001

Post-operative pain

The WHO estimated that 313 million surgeries are performed each year, and a considerable proportion of patients experience undesirable levels of postoperative pain. A poorly controlled postoperative pain may delay recovery time and the patients may suffer chronic pain that may impair their quality-of-life, causing prolonged duration of opioid use, and higher health-care costs. A US survey showed that 80% of the patients who underwent surgeries experience poorly managed postoperative pain. Opioids (such as morphine, oxycodone and fentanyl) are the mainstay analgesia for postoperative pain but often associated with side effects such as pruritus, urinary retention, constipation, and respiratory depression, as well as risks of substance abuse. Opioid-involved deaths in the US was 49,860 in 2019 which raised the general public’s concern regarding this issue.

Nalbuphine, a mixed kappa agonist and mu antagonist is developed as an attempt to address opiate-related side effects without the risks involving substance dependence while providing moderate to severe pain relief. Due to its short-acting effect, patients need to be given nalbuphine every 4-6 hours. This may cause blood concentration of nalbuphine to temporarily overshoot the therapeutic window, leading to nausea, dizziness, and vomiting.

How LT1001 can help?

LT1001 is the world's first analgesic injection that offers analgesic effect up to 7 days taking the advantages of nalbuphine. This allows LT1001 to maintain a constant analgesic effect without triggering unwanted side effects while addressing opioid-related issues. LT1001 improves the quality of postoperative care and facilitates rehabilitation to shorten hospital stay.

The API of LT1001, dinalbuphine sebacate (DNS), is a hydrophobic compound containing two nalbuphine molecules joined by sebacoyl ester. The hydrophobic depo environment allows DNS to be slowly released into circulation after IM injection and to be rapidly hydrolyzed by esterases to release nalbuphine. LT1001 produces sustained plasma concentration of nalbuphine by prolonging its half-life, achieving a sustained analgesic effect.

LT1001

Development progress

LT1001 received marketing approval in Taiwan from Taiwan FDA in 2017 and is sold as Naldebain®. LT1001 received approval from Singapore’s HSA in 2020. The development and commercial rights for mainland China and ASEAN countries were granted to Jamincare and AMed, respectively. Registration process is ongoing in Ukraine, Korea, Malaysia, and Thailand.

Clinical Trials

  • Stage
  • Description
  • Region
  • Status
  • Link
  • Stage :
    Phase 1 (SDE-002)
  • Description :
    PK comparison of SDE to nalbuphine
  • Region :
    Taiwan
  • Status :
    Completed
  • Link :
    TBA
  • Stage :
    Phase 1 (LT1001-103)
  • Description :
    PK and bioavailability between SDE and nalbuphine
  • Region :
    Taiwan
  • Status :
    Completed
  • Link :
    TBA
  • Stage :
    Phase 3 (SDE-2-001)
  • Description :
    Safety and efficacy of SDE on post-hemorrhoidectomy pain
  • Region :
    Taiwan
  • Status :
    Completed
  • Link :
    TBA
  • Stage :
    Phase 3 (SNFB3-2020001)
  • Description :
    Safety and efficacy of SDE on post-operative pain
  • Region :
    China
  • Status :
    Ongoing
  • Link :
    TBA