Technology

DISCOVERING OUR LEAD COMPOUND

Based on overall chemical stability, efficacy, negligible cardiovascular effects, and onset profiles, ATLX-0199 (D-Cystine diME) was selected as the lead compound for clinical development, with back-up compounds available.  ATLX-0199 safely stimulates opioid-depressed respiratory drive without interfering with opioid-induced analgesia.

PLATFORM/PIPELINE

Lead compound ATLX-0199 ready for clinical development, with platform molecules available

HOW IT WORKS

ATLX-0199, an active thiol-based compound from our platform of novel drugs, reverses opioid-induced side effects such as OIRD while preserving pain relief:

  • ATLX-0199 targets molecular pathways, modulating signals downstream from activated opioid receptors
  • Concept validated by extensive NIH-supported research/data
  • Atelerix is developing ATLX-0199 and other compounds in its pipeline to treat the range of opioid-induced side effects; first focus is OIRD in the hospital surgical setting

AVAILABLE DATA

In-vitro & in-vivo data show compelling pre-clinical proof of concept

ATLX-0199 (D-Cystine diME)

  • ATLX-0199 increases minute ventilation and overcomes opioid-induced respiratory depression.
  • ATLX-0199 (D-Cystine diME) reverses the respiratory depression and V/Q mismatch after 10 mg/kg IV morphine in conscious rats.
  • ATLX-0199 (D-Cystine diME) does not negatively impact the analgesic actions of morphine in freely-moving rats.

Additional data on opioid withdrawal response, tolerance, motility, modulation of addiction and co-administration with naloxone is available under CDA

PRE-CLINICAL PROOF OF CONCEPT

ATLX-0199 increases minute ventilation and overcomes opioid-induced respiratory depression

Minute ventilation (VE) is the total volume of gas entering (or leaving) the lung per/min

It is equal to the tidal volume (TV) multiplied by the respiratory frequency rate (f).

VE = TV x f

No toxicity observed to date at maximal effective doses

PRE-CLINICAL PROOF OF CONCEPT

ATLX-0199 reverses the respiratory depression and V/Q mismatch after 10 mg/kg IV morphine in conscious rats

Studied blood gas parameters include:

Blood pH

Increases in CO2

Hemoglobin saturation

Oxygen imbalance between lungs and arteries

PRE-CLINICAL PROOF OF CONCEPT

ATLX-0199 does not negatively impact the analgesic actions of morphine in freely-moving rats