Unmet Need

Healthcare professionals frequently prescribe more than one therapeutic agent, each with a different mode of action, to address complexity of any given disease. Multi-modal therapy has demonstrated improved outcomes across a range of conditions – including pain – and it is recommended as the standard of care in many therapeutic areas. However, this approach creates a need for multiple prescriptions to combine multiple drugs – increasing the overall cost – and often resulting in an arduous trial and error process, for both physicians and patients, to achieve an optimal ratio with acceptable efficacy and tolerability profile.

 

Xgene’s proprietary linker technology, tailored to the recognized profiles of specific existing and newly discovered drugs, overcomes the challenges of multimodal drug combination approach and offers potentially better, safer, and more efficient treatments.

 

Acute and chronic pain conditions, the current clinical focus of Xgene, are prominent in the US and across the globe. Acute pain, that can last for days or few weeks, usually results from a medical procedure or an injury and frequently requires analgesic intervention. Chronic pain, defined as daily pain for more than 3 months, can lead to impaired memory, cognition, and attention, sleep disturbances, reduced physical function, and work absenteeism. Wide-spread use of opioids to treat pain regardless of its origin has led to a declaration of a public health crisis in the US. XG005, a non-opioid dual-acting conjugated prodrug in development in oral and topical formulations, has a potential to greatly reduce if not eliminate the need for use of opioids in many painful conditions.

Technology

Patentable New

Chemical Entity

Xgene utilizes a novel proprietary chemical conjugation method to link different moieties with complementary mechanisms of action. This technology, unlike taking the two drugs together or in a fixed-dose-combination, enables the fine-tuning of the linker cleavage rate thus modifying dissolution, absorption, metabolism, and pharmacokinetic profiles of the linked moieties and creating a single, multimodal, patentable molecule with distinct therapeutic properties. Animal studies of XG005, a proprietary dual-acting prodrug conjugate, have demonstrated an improved analgesic efficacy and a better safety profile when compared with the two parent drugs given in combination.

Values

Synchronized PK Profiles between Drug A and Drug B

A reduction in GI and Central Nervous System side effects (headache, dizziness, sleepiness, confusion, etc.)

Expanded indications of parent drug products

Pipeline

PRODUCT CANDIDATE

DISCOVERY

PRECLINICIAL

PHASE 1

PHASE 2

PHASE 3

RIGHTS

ACUTE PAIN

XG005

Oral Tablet

Dual-acting prodrug conjugate of an NSAID and a gabapentinoid scheduled to enter Phase II/III program following FDA regulatory pathway in the US in 2023. It has demonstrated superior analgesic efficacy and side effects profile in preclinical studies and improved PK characteristics in Phase I trials as compared to the parent drugs.

Global

CHRONIC PAIN

XG005

Oral Tablet

Dual-acting prodrug conjugate of an NSAID and a gabapentinoid scheduled to enter phase II trial following Class 1 regulatory pathway in China in 2022. It has demonstrated superior efficacy and side effects profile in preclinical studies and improved PK characteristics in Phase I study as compared to the parent drugs.

Global

CHRONIC PAIN

XG004

Topical Gel

Dual-acting prodrug conjugate of an NSAID and a gabapentinoid (stereoisomer of XG005) with high transdermal penetration properties. It has demonstrated superior analgesic efficacy compared with an oral administration of a parent drug in animal studies. A Phase I/II trial, including exploratory analgesic endpoints, in patients with Osteoarthritis has commenced in Australia..

Global

CHRONIC PAIN, METASTATIC BONE PAIN

XG2002

Novel Target

TRPM8 channel blocker - IND-enabling preclinical studies are ongoing.

Global Excluding Japan

HEADACHE

XG043

Oral Tablet

Dual-acting prodrug conjugate of a modulator of α2δ subunit of calcium channel and a GABAb agonist in lead optimization stage.

Global

Pipeline

ACUTE PAIN

XG005

Oral Tablet

Phase 2

 

Dual-acting prodrug conjugate of an NSAID and a gabapentinoid scheduled to enter Phase II/III program following FDA regulatory pathway in the US in 2023. It has demonstrated superior analgesic efficacy and side effects profile in preclinical studies and improved PK characteristics in Phase I trials as compared to the parent drugs.

Global rights

CHRONIC PAIN

XG005

Oral Tablet

Phase 2

 

Dual-acting prodrug conjugate of an NSAID and a gabapentinoid scheduled to enter phase II trial following Class 1 regulatory pathway in China in 2022. It has demonstrated superior efficacy and side effects profile in preclinical studies and improved PK characteristics in Phase I study as compared to the parent drugs.

Global rights

CHRONIC PAIN

XG004

Topical Gel

Phase 1b/2a

 

Dual-acting prodrug conjugate of an NSAID and a gabapentinoid (stereoisomer of XG005) with high transdermal penetration properties. It has demonstrated superior analgesic efficacy compared with an oral administration of a parent drug in animal studies. A Phase I/II trial, including exploratory analgesic endpoints, in patients with Osteoarthritis has commenced in Australia..

Global rights

CHRONIC PAIN, METASTATIC BONE PAIN

XG2002

Novel Target

Discovery/Pre-clinical

 

TRPM8 channel blocker – IND-enabling preclinical studies are ongoing.

Global Excluding Japan rights

HEADACHE

XG043

Oral Tablet

Discovery

 

Dual-acting prodrug conjugate of a modulator of α2δ subunit of calcium channel and a GABAb agonist in lead optimization stage.

Global rights