4E Therapeutics is developing a pipeline of non-opioid therapeutic assets to target pain.

We currently have 3 areas of focus:

Phase

Discovery

IND-Enabling

Phase 1

Phase 2

Phase 3

Neuropathic Pain
4ET1103

IND-Enabling Completed

50%
Migraine Pain
4ET2124

IND-Enabling

30%
Acute Pain
MNK-eIF4E

Discovery

11%
Neuropathic Pain

4E Therapeutics has completed our medicinal chemistry optimization program in which over 150 proprietary, small molecule MNK inhibitors were synthesized and evaluated, leading to the discovery of a cohort of peripherally-restricted, orally-bioavailable compounds.

Phase

Discovery

IND-Enabling

Phase 1

Phase 2

Phase 3

4ET1103

Selected as lead compound

IND-Enabling Completed

50%

Having met our stringent preclinical safety and efficacy criteria, 4ET1103 is highly efficacious in multiple animal models of pain and is well-tolerated in rodents and dogs. Significantly, 4ET1103 blocks evoked MNK activity in human dorsal root ganglion neurons from organ donors, underscoring its translational potential.

4ET1103 has completed IND-enabling studies and IND application to be submitted Q4 2023.
Migraine Pain

4E Therapeutics research shows that the MNK-eIF4E signaling pathway is implicated in migraine, and that disrupting this pathway is a promising strategy for inhibiting migraine pain.

Phase

Discovery

IND-Enabling

Phase 1

Phase 2

Phase 3

4ET2124

Selected as lead compound

IND-Enabling

30%

Building upon these discoveries, 4E is developing small molecule MNK inhibitors into next generation drugs for the treatment of migraine. 4ET2124 has been selected as a clinical candidate for the treatment of migraine pain, with 4ET2104 positioned as backup. Both compounds have excellent in vitro safety profiles and are efficacious across multiple animal models of migraine.

4ET2124 and 4ET2104 are ready to begin IND-Enabling studies.
Acute Pain

Peripherally restricted MNK inhibitor

Phase

Discovery

IND-Enabling

Phase 1

Phase 2

Phase 3

MNK-eIF4E Signaling Pathway

Discovery

11%

Our approach employs non-brain penetrant small molecules to selectively inhibit MNK. Peripherally-restricted therapeutics are advantageous because they are devoid of central-nervous-system side effects, such as impaired cognitive function and physical dependence.

A lead compound will be selected in 2024.