Protein / target

Voltage-dependent L-type calcium channel subunit beta-1

CACNB1Q02641Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
7
Approved medicines
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

High voltage-gated calcium channel activity

Primary system

Musculoskeletal system

Strongest disease association

epilepsy

Clinical evidence · score 0.61

Therapeutic maturity

Clinically validated target

7 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

7 approved · 2 in clinical development

30 linked trials

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function

Regulatory subunit of L-type calcium channels (PubMed:1309651, PubMed:15615847, PubMed:8107964). Regulates the activity of L-type calcium channels that contain CACNA1A as pore-forming subunit (By similarity). Regulates the activity of L-type calcium channels that contain CACNA1C as pore-forming subunit and increases the presence of the channel complex at the cell membrane (PubMed:15615847). Required for functional expression L-type calcium channels that contain CACNA1D as pore-forming subunit (PubMed:1309651). Regulates the activity of L-type calcium channels that contain CACNA1B as pore-forming subunit (PubMed:8107964)

Subcellular location

Cell membrane, sarcolemmaCell membrane
Domains and Gene Ontology detail (14)

Domains & features

SH3

Gene Ontology

  • Cplasma membrane
  • Csynapse
  • CT-tubule
  • Cvoltage-gated calcium channel complex
  • Fcalcium channel regulator activity
  • Fhigh voltage-gated calcium channel activity
  • Fvoltage-gated calcium channel activity
  • Pcalcium ion transmembrane transport
  • Pcalcium ion transport
  • Pcellular response to amyloid-beta
  • Pchemical synaptic transmission
  • Ppositive regulation of muscle contraction

598 aa · 66 kDa · 3 isoforms

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Synaptic signallingGO · ReactomeIon channel gatingGOMuscle contractionGO
View supporting evidence

Synaptic signalling

  • ·synapse
  • ·chemical synaptic transmission
  • ·Presynaptic depolarization and calcium channel opening

Ion channel gating

  • ·calcium ion transmembrane transport
  • ·regulation of calcium ion transmembrane transport via high voltage-gated calcium channel

Muscle contraction

  • ·positive regulation of muscle contraction
View underlying pathways (5)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.

CACNA2…CACNG1CACNA1SCACNA1DCACNA1CCACNA1BCACNA2…CACNB2CACNB3CACNA2…CACNB1

10 strongest partners — larger node and heavier line mean higher confidence

Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.

Drugs targeting this protein

1

Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.

gabapentin
ApprovedModulator

Voltage-gated calcium channel modulator

Appears in clinical studies involving Seizure, epilepsy, Focal-onset seizure, restless legs syndrome

Acts on a complex — shared with CACNB4, CACNG4, CACNG3 +22 more · 1 of 26 recorded protein targets — broad pharmacology

ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.

Translational evidence

Open Targets 26

Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

epilepsy1.00

Clinical · overall 0.61

neuropathic pain0.99

Clinical · overall 0.60

fibromyalgia0.99

Clinical · overall 0.60

Seizure0.99

Clinical · overall 0.60

restless legs syndrome0.97

Clinical · overall 0.59

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

postherpetic neuralgia0.57

Clinical

anxiety disorder0.57

Clinical

neuralgia0.56

Clinical

Focal-onset seizure0.52

Clinical

spinal cord injury0.49

Clinical

Show all associations
epilepsy0.61
neuropathic pain0.60
fibromyalgia0.60
Seizure0.60
restless legs syndrome0.59
postherpetic neuralgia0.57
anxiety disorder0.57
neuralgia0.56
Focal-onset seizure0.52
spinal cord injury0.49

Open Targets ranks 382 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.

Known drugs · 10 total

TERODILINE HYDROCHLORIDEUnknown
TERODILINEApproval

Polyuria · Urinary incontinence

SULOCTIDILApproval

cardiovascular disorder

PHLOROGLUCINOLApproval

gastrointestinal disease · urinary system disorder · renal colic

GABAPENTIN ENACARBILApproval

restless legs syndrome · neuralgia · Sleep disturbance

PREGABALINApproval

Seizure · neuropathic pain · fibromyalgia

GABAPENTINApproval

Seizure · epilepsy · Focal-onset seizure

IMAGABALINPhase 3

generalized anxiety disorder

BEPRIDILApproval

cardiovascular disorder

ATAGABALINPhase 2

insomnia

Tractability

SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt loc med confPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule Binder

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.

Show remaining trials (24)

COMPLETED · via gabapentin · NCT02330094

COMPLETED · via gabapentin · NCT00279487

COMPLETED · via gabapentin · NCT00058890

RECRUITING · via gabapentin · NCT04724252

COMPLETED · via gabapentin · NCT00218374

UNKNOWN · via gabapentin · NCT00209872

ClinicalTrials.gov via the drug-target graph.

Forefront confidence

Synthesis

Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.

epilepsyModerately supported
0.75
agreement 0.590.90
Clinical100%Literature0%

Open Targets aggregate 0.61 · 2 independent evidence families

neuropathic painModerately supported
0.74
agreement 0.580.91
Clinical100%

Open Targets aggregate 0.60 · 1 independent evidence family

fibromyalgiaModerately supported
0.74
agreement 0.580.91
Clinical100%

Open Targets aggregate 0.60 · 1 independent evidence family

SeizureModerately supported
0.74
agreement 0.580.91
Clinical100%

Open Targets aggregate 0.60 · 1 independent evidence family

restless legs syndromeModerately supported
0.72
agreement 0.560.89
Clinical100%

Open Targets aggregate 0.59 · 1 independent evidence family

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.

What's happening now

30

Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.

  1. Label change2026-07-22

    Label change: GABAPENTIN (ANDA217995)

    fda · regulatory · fda · via gabapentin

  2. Label change2026-07-17

    Label change: GABAPENTIN (ANDA203934)

    fda · regulatory · fda · via gabapentin

  3. Label change2026-07-16

    Label change: GABAPENTIN (ANDA075428)

    fda · regulatory · fda · via gabapentin

  4. Label change2026-06-25

    Label change: GABAPENTIN (ANDA077661)

    fda · regulatory · fda · via gabapentin

  5. Regulatory approval2026-06-23

    Approval: GABAPENTIN (ANDA203611)

    fda · regulatory · fda · via gabapentin

  6. Label change2024-12-27

    Label change: GABAPENTIN (ANDA217995)

    fda · regulatory · fda · via gabapentin

  7. Label change2024-12-16

    Label change: GABAPENTIN (ANDA075428)

    fda · regulatory · fda · via gabapentin

  8. Label change2024-07-08

    Label change: GABAPENTIN (ANDA075428)

    fda · regulatory · fda · via gabapentin

  9. Label change2024-07-08

    Label change: GABAPENTIN (ANDA075428)

    fda · regulatory · fda · via gabapentin

  10. Regulatory approval2024-01-24

    Approval: GABAPENTIN (ANDA203934)

    fda · regulatory · fda · via gabapentin

  11. Label change2023-09-21

    Label change: GABAPENTIN (ANDA077661)

    fda · regulatory · fda · via gabapentin

  12. Label change2023-09-21

    Label change: GABAPENTIN (ANDA077661)

    fda · regulatory · fda · via gabapentin

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.