BL-1110 was shown in preclinical studies to enhance analgesic effect of morphine while reducing negative side effects
BL-1110 may also be developed for scleroderma
Neuropathic pain is caused by damage or diseases affecting the nervous
system, and usually does not respond well to regular painkillers. One of
the most potent drugs for the treatment of neuropathic pain is morphine;
however, its efficacy is often significantly limited due to the body’s
development of tolerance to the drug, as well as its severe side
effects. Morphine can create neuroinflammation in the central nervous
system, which has been linked to the suppression of morphine analgesia,
as well as the enhancement of morphine-induced tolerance, dependence and
reward associated with drug abuse. Recent studies show part of these
neuroinflammatory effects are triggered by the interaction of morphine
with glial cells, which are highly prevalent in the central nervous
system. BL-1110, which was invented by Prof.
BL-1110 is a small molecule that targets the critical TLR4/MD-2 complex formation, thus preventing the binding of morphine to the TLR4 receptor in glial cells. BL-1110 is administered orally, together with morphine or other opioids. In preclinical studies in rats, BL-1110 was shown to enhance the effects of morphine. Furthermore, the studies show the drug penetrates the blood-brain barrier and reaches the central nervous system with high efficiency, that it is safe for use and that it does not induce adverse effects at doses that are much higher than the effective dose.
“BL-1110 works through a novel mechanism-of-action, based on our recent
discovery that opioids, such as morphine, cause the activation of glial
cells. This glial activation results in the release of pro-inflammatory
factors, which suppress the desired opioid-induced neuronal analgesic
effect, thereby reducing the efficacy of the opioid. Furthermore,
evidence suggests that glial activation contributes to the development
of opioid tolerance, dependence and abuse,” explained Prof.
“Neuropathic pain is a major health problem affecting the quality of life of millions of people around the globe on a daily basis. Despite its widespread occurrence, it is notoriously difficult to treat. Opioids, such as morphine, are a potent option for the treatment of neuropathic pain, but they are generally not used as a first-line treatment due to the considerable risk of adverse side effects, tolerance and dependence.
BL-1110 offers the possibility of mitigating morphine tolerance and side
effects while enhancing the analgesic effect. This drug could offer a
real breakthrough for the treatment of this challenging and persistent
pathology. We are therefore very pleased to in-license this drug and
continue its development,” said Dr.
About Neuropathic Pain
Neuropathic pain develops as a result of damage to, or dysfunction of, the nervous system and is often a chronic condition. The causes of neuropathic pain can include shingles, diabetes and cancer, but in many cases the underlying pathology is not completely understood. Neuropathic pain does not usually respond to regular pain killers, and can be very difficult to treat; only approximately 50% of patients achieve even partial relief. Annual sales of prescription drugs for neuropathic pain exceed
BL-1110, developed by BioLineRx under its Early Development Program and previously known as EDP 34, is an orally-administered small molecule designed to block the binding of morphine to the toll-like receptor-4 (TLR4) on glial cells. Research shows that besides the activity of opioids on opioid receptors in the neurons, opioids cause activation of glial cells via the TLR4 signaling pathway, which activation results in the release of cytokines and other pro-inflammatory factors that suppress the desired opioid-induced neuronal analgesic effect, thereby reducing the efficacy of the opioid. Furthermore, evidence suggests that glial activation by opioids contributes to the negative side effects of opioid therapy, such as tolerance, dependence and reward associated with drug abuse. BL-1110 prevents morphine- binding to TLR4 receptors on glial cells, resulting in an enhanced analgesic effect and reduced side effects. BL-1110 was invented by Prof.
BioLineRx is a publicly-traded, clinical-stage biopharmaceutical company dedicated to identifying, in-licensing and developing promising therapeutic candidates. The Company in-licenses novel compounds primarily from academic institutions and biotech companies based in
BioLineRx’s current portfolio consists of a variety of clinical and
pre-clinical projects, including: BL-1040 for prevention of pathological
cardiac remodeling following a myocardial infarction, which has been
out-licensed to Bellerophon BCM (f/k/a
For more information on BioLineRx, please visit www.biolinerx.com
or download the investor relations mobile device app, which allows users
access to the Company’s
Various statements in this release concerning BioLineRx’s future
expectations, including specifically those related to the development
and commercialization of BL-1110, constitute “forward-looking
statements” within the meaning of the Private Securities Litigation
Reform Act of 1995. These statements include words such as “may,”
“expects,” “anticipates,” “believes,” and “intends,” and describe
opinions about future events. These forward-looking statements involve
known and unknown risks and uncertainties that may cause the actual
results, performance or achievements of BioLineRx to be materially
different from any future results, performance or achievements expressed
or implied by such forward-looking statements. Some of these risks are:
changes in relationships with collaborators; the impact of competitive
products and technological changes; risks relating to the development of
new products; and the ability to implement technological improvements.
These and other factors are more fully discussed in the “Risk Factors”
section of BioLineRx’s most recent annual report on Form 20-F filed with
Tiberend Strategic Advisors, Inc.
Joshua Drumm, Ph.D., +1-212-375-2664
Andrew Mielach, +1-212-375-2694
Tsipi Haitovsky, Public Relations