AM-102
From Wikipedia, the free encyclopedia
- NKCC1 inhibitor
- Small molecule
- none
| Clinical data | |
|---|---|
| Other names | AM102; AM-102 (Altamira Therapeutics) |
| Drug class |
|
| ATC code |
|
| Pharmacokinetic data | |
| Bioavailability | Not applicable |
| Metabolism | Unknown |
| Excretion | Unknown |
AM-102 (also known as AM102) is an investigational small molecule drug candidate being developed by Altamira Therapeutics for the treatment of tinnitus.[1]
According to company statements and patent filings, AM-102 acts as an inhibitor of the sodium–potassium–chloride co-transporter 1 (NKCC1), a mechanism thought to modulate neuronal chloride homeostasis involved in tinnitus perception.[2]
The compound was developed by Altamira Therapeutics (formerly Auris Medical) in collaboration with King’s College London as part of a program to identify small-molecule drugs for tinnitus.[3]
As of February 2024, there have been no publicly announced clinical trials or active development updates for AM-102 in tinnitus.[4]
Mechanism of action
AM-102 is reported to act via inhibition of the Na⁺K⁺2Cl⁻ co-transporter 1 (NKCC1), a transporter involved in chloride homeostasis in auditory cells.[2]
By inhibiting NKCC1, it is hypothesised that the excitatory-inhibitory balance in inner-ear sensory neurons may be restored, potentially reducing the perception of tinnitus.[2][5]
A relevant patent application describes the concept of NKCC1 antagonists for tinnitus, citing a link between injury-induced down-regulation of KCC2 (the chloride–potassium co-transporter) and tinnitus.[2]
Preclinical and clinical data
Preclinical studies
In animal models of noise-induced tinnitus (Mongolian gerbils), compounds of the NKCC1 inhibitor class significantly reduced behavioural markers of tinnitus and preserved inner hair-cell ribbon synapses.[6]
Clinical development
While AM-102 specifically has limited disclosed trial data, a related compound AM‑101 (also from Auris Medical/Altamira) underwent a Phase-2 intratympanic study in tinnitus after noise trauma or otitis media.[7][8]
The AM-101 study (0.81 mg/ml) showed statistically significant improvements for tinnitus loudness, annoyance, sleep disturbances and tinnitus impact, though the primary endpoint (minimum masking level) was not met.[7][9]
Patent and intellectual property
A patent application (ES2862673T3) describes the use of NKCC1 modulators (including bumetanide derivatives) for tinnitus treatment via chloride-transport modulation in auditory sensory cells. An allowed European patent application (NKCC1 inhibitor for tinnitus) was noted in Switzerland for Auris Medical in January 2020.[10]