Rob Kirby PhD, COO and Eddy Stevens PhD, CSO
Ion channels remain some of the most important targets in drug discovery, particularly across neuroscience, pain, inflammation and cardiovascular disease. While many ion channel therapeutics have historically been developed using small molecules, biologic modalities are gaining attention as researchers explore new approaches for challenging targets where subtype selectivity and mechanism of action are critical.
Biologic modalities may offer opportunities to achieve levels of subtype selectivity that can be difficult to obtain using traditional small molecules, particularly across closely related ion channel family members. This may enable more precise modulation of disease-relevant targets while potentially reducing unwanted off-target activity.
Approaches currently under investigation include:
These modalities offer exciting opportunities to explore alternative mechanisms of ion channel modulation, while also introducing distinct scientific and technical challenges.
In ion channel biologics discovery, early screening often relies on binding assays to identify molecules that recognise the target.
However, binding affinity does not predict functional effect. Compounds with similar affinity can produce inhibition, potentiation, altered gating, or no detectable activity.
Electrophysiology is, therefore, essential to confirm whether binding translates into functional modulation of channel activity.
Compared with traditional small molecules, biologics targeting ion channels may exhibit complex pharmacology measured using electrophysiology, including:
Robust and rigorously designed electrophysiology assays are an important component of biologics discovery and characterisation.
Approaches such as our automated and manual patch clamp ion channel screening services can help assess:
Importantly, assay design can have a significant impact on the measured activity of biologics as ion channel modulators. Factors such as sample handling, voltage protocol, stimulation frequency incubation time and channel state can all influence observed pharmacology. Tailored electrophysiology protocols are therefore often required to fully characterise biologic activity and mechanism of action.
This functional understanding is often critical for interpreting candidate behaviour and supporting decision-making throughout discovery.
Interest in biologic and peptide-based ion channel therapeutics continues to expand across areas including pain, migraine, neuroinflammation and neurodegeneration.
Examples of targets under active investigation include:
In these programmes, subtle differences in pharmacology may have important translational implications, making detailed functional characterisation especially valuable during candidate evaluation.
Some of the most selective ion channel modulators identified to date originated from venom peptides derived from cone snails, spiders and scorpions. One notable example is ziconotide, a CaV2.2-targeting peptide derived from cone snail venom and approved for severe chronic pain.
These discoveries continue to demonstrate the potential of biologic and peptide-based approaches for ion channel modulation.
Why choose Metrion as your CRO for ion channel biologics discovery
As a specialist ion channel CRO, Metrion supports biologics-focused discovery programmes through:
Our scientists work collaboratively with clients to develop assay strategies aligned to the biology of each target and the characteristics of each modality.
This flexible, science-led approach enables robust evaluation of complex ion channel pharmacology across a broad range of biologic programmes.
Biologic modalities are expanding the range of approaches available for ion channel drug discovery and opening new possibilities for challenging targets where selectivity and mechanism remain important considerations.
As these programmes continue to evolve, high-quality functional electrophysiology will remain essential for understanding biologic modulation of ion channels and generating pharmacologically meaningful data.
While binding assays and other target engagement approaches provide valuable information, electrophysiology remains the most direct measure of ion channel function. This enables researchers to characterise how biologics influence channel activity in real time and generate mechanistic insightsThrough specialist expertise in ion channel pharmacology, assay development and electrophysiology, Metrion continues to support researchers advancing next-generation ion channel therapeutics.
Find out how our expert scientific team can help advance your biologics project.
Rob Kirby PhD, COO and Eddy Stevens PhD, CSO
Ion channels remain some of the most important targets in drug discovery, particularly across neuroscience, pain, inflammation and cardiovascular disease. While many ion channel therapeutics have historically been developed using small molecules, biologic modalities are gaining attention as researchers explore new approaches for challenging targets where subtype selectivity and mechanism of action are critical.
Biologic modalities may offer opportunities to achieve levels of subtype selectivity that can be difficult to obtain using traditional small molecules, particularly across closely related ion channel family members. This may enable more precise modulation of disease-relevant targets while potentially reducing unwanted off-target activity.
Approaches currently under investigation include:
These modalities offer exciting opportunities to explore alternative mechanisms of ion channel modulation, while also introducing distinct scientific and technical challenges.
In ion channel biologics discovery, early screening often relies on binding assays to identify molecules that recognise the target.
However, binding affinity does not predict functional effect. Compounds with similar affinity can produce inhibition, potentiation, altered gating, or no detectable activity.
Electrophysiology is, therefore, essential to confirm whether binding translates into functional modulation of channel activity.
Compared with traditional small molecules, biologics targeting ion channels may exhibit complex pharmacology measured using electrophysiology, including:
Robust and rigorously designed electrophysiology assays are an important component of biologics discovery and characterisation.
Approaches such as our automated and manual patch clamp ion channel screening services can help assess:
Importantly, assay design can have a significant impact on the measured activity of biologics as ion channel modulators. Factors such as sample handling, voltage protocol, stimulation frequency incubation time and channel state can all influence observed pharmacology. Tailored electrophysiology protocols are therefore often required to fully characterise biologic activity and mechanism of action.
This functional understanding is often critical for interpreting candidate behaviour and supporting decision-making throughout discovery.
Interest in biologic and peptide-based ion channel therapeutics continues to expand across areas including pain, migraine, neuroinflammation and neurodegeneration.
Examples of targets under active investigation include:
In these programmes, subtle differences in pharmacology may have important translational implications, making detailed functional characterisation especially valuable during candidate evaluation.
Some of the most selective ion channel modulators identified to date originated from venom peptides derived from cone snails, spiders and scorpions. One notable example is ziconotide, a CaV2.2-targeting peptide derived from cone snail venom and approved for severe chronic pain.
These discoveries continue to demonstrate the potential of biologic and peptide-based approaches for ion channel modulation.
Why choose Metrion as your CRO for ion channel biologics discovery
As a specialist ion channel CRO, Metrion supports biologics-focused discovery programmes through:
Our scientists work collaboratively with clients to develop assay strategies aligned to the biology of each target and the characteristics of each modality.
This flexible, science-led approach enables robust evaluation of complex ion channel pharmacology across a broad range of biologic programmes.
Biologic modalities are expanding the range of approaches available for ion channel drug discovery and opening new possibilities for challenging targets where selectivity and mechanism remain important considerations.
As these programmes continue to evolve, high-quality functional electrophysiology will remain essential for understanding biologic modulation of ion channels and generating pharmacologically meaningful data.
While binding assays and other target engagement approaches provide valuable information, electrophysiology remains the most direct measure of ion channel function. This enables researchers to characterise how biologics influence channel activity in real time and generate mechanistic insightsThrough specialist expertise in ion channel pharmacology, assay development and electrophysiology, Metrion continues to support researchers advancing next-generation ion channel therapeutics.
Find out how our expert scientific team can help advance your biologics project.
Rob Kirby PhD, COO and Eddy Stevens PhD, CSO
Ion channels remain some of the most important targets in drug discovery, particularly across neuroscience, pain, inflammation and cardiovascular disease. While many ion channel therapeutics have historically been developed using small molecules, biologic modalities are gaining attention as researchers explore new approaches for challenging targets where subtype selectivity and mechanism of action are critical.
Biologic modalities may offer opportunities to achieve levels of subtype selectivity that can be difficult to obtain using traditional small molecules, particularly across closely related ion channel family members. This may enable more precise modulation of disease-relevant targets while potentially reducing unwanted off-target activity.
Approaches currently under investigation include:
These modalities offer exciting opportunities to explore alternative mechanisms of ion channel modulation, while also introducing distinct scientific and technical challenges.
In ion channel biologics discovery, early screening often relies on binding assays to identify molecules that recognise the target.
However, binding affinity does not predict functional effect. Compounds with similar affinity can produce inhibition, potentiation, altered gating, or no detectable activity.
Electrophysiology is, therefore, essential to confirm whether binding translates into functional modulation of channel activity.
Compared with traditional small molecules, biologics targeting ion channels may exhibit complex pharmacology measured using electrophysiology, including:
Robust and rigorously designed electrophysiology assays are an important component of biologics discovery and characterisation.
Approaches such as our automated and manual patch clamp ion channel screening services can help assess:
Importantly, assay design can have a significant impact on the measured activity of biologics as ion channel modulators. Factors such as sample handling, voltage protocol, stimulation frequency incubation time and channel state can all influence observed pharmacology. Tailored electrophysiology protocols are therefore often required to fully characterise biologic activity and mechanism of action.
This functional understanding is often critical for interpreting candidate behaviour and supporting decision-making throughout discovery.
Interest in biologic and peptide-based ion channel therapeutics continues to expand across areas including pain, migraine, neuroinflammation and neurodegeneration.
Examples of targets under active investigation include:
In these programmes, subtle differences in pharmacology may have important translational implications, making detailed functional characterisation especially valuable during candidate evaluation.
Some of the most selective ion channel modulators identified to date originated from venom peptides derived from cone snails, spiders and scorpions. One notable example is ziconotide, a CaV2.2-targeting peptide derived from cone snail venom and approved for severe chronic pain.
These discoveries continue to demonstrate the potential of biologic and peptide-based approaches for ion channel modulation.
Why choose Metrion as your CRO for ion channel biologics discovery
As a specialist ion channel CRO, Metrion supports biologics-focused discovery programmes through:
Our scientists work collaboratively with clients to develop assay strategies aligned to the biology of each target and the characteristics of each modality.
This flexible, science-led approach enables robust evaluation of complex ion channel pharmacology across a broad range of biologic programmes.
Biologic modalities are expanding the range of approaches available for ion channel drug discovery and opening new possibilities for challenging targets where selectivity and mechanism remain important considerations.
As these programmes continue to evolve, high-quality functional electrophysiology will remain essential for understanding biologic modulation of ion channels and generating pharmacologically meaningful data.
While binding assays and other target engagement approaches provide valuable information, electrophysiology remains the most direct measure of ion channel function. This enables researchers to characterise how biologics influence channel activity in real time and generate mechanistic insightsThrough specialist expertise in ion channel pharmacology, assay development and electrophysiology, Metrion continues to support researchers advancing next-generation ion channel therapeutics.
Find out how our expert scientific team can help advance your biologics project.