MAPT

# MAPT (Microtubule-Associated Protein Tau) — Target Profile ## Overview Microtubule-Associated Protein Tau (MAPT) is central to Alzheimer's disease and tauopathies. Tau stabilizes microtubules but hyperphosphorylation causes aggregation into neurofibrillary tangles. Six isoforms (3R/4R) exist with distinct disease associations. Tau pathology correlates with cognitive decline more strongly than amyloid plaques, making it a prime therapeutic target. **Target class: Structural Protein** — Tau is an intrinsically disordered protein that adopts pathological conformations during disease. While historically challenging to drug, cryo-EM structures of disease-specific tau filament folds have enabled conformation-selective therapeutic approaches. ## Druggability Analysis This target has a **medium druggability** profile. Multiple therapeutic modalities are being explored including anti-tau antibodies, aggregation inhibitors, antisense oligonucleotides (ASOs), and kinase inhibitors targeting tau phosphorylation. **Druggability score:** 0.65 (65th percentile) — Target shows moderate druggability with multiple active clinical programs. ## Clinical Pipeline **Phase 3:** - **LMTX (TRx0237)** — Tau aggregation inhibitor for Alzheimer's disease **Phase 2:** - **Semorinemab** — Anti-tau antibody for Alzheimer's disease - **Bepranemab** — Anti-tau antibody targeting mid-domain tau **Phase 1/Preclinical:** - **Tilavonemab** — Anti-tau antibody (N-terminal) - **BIIB080 (IONIS-MAPTRx)** — Antisense oligonucleotide reducing tau expression ## Structural Biology 134 PDB structures available, including cryo-EM structures of disease-specific tau filament folds. AlphaFold predicted structure also available. Cryo-EM revealed that different tauopathies feature distinct filament conformations, enabling conformation-selective drug design. ## SciDEX Research Context - One of the most studied targets in the neurodegeneration portfolio - Strong knowledge graph connectivity to Alzheimer's disease pathways - Multiple hypotheses in the SciDEX Exchange involve tau-related mechanisms

Score: 0.365 Price: $0.36 Medium Druggability Status: active Wiki: MAPT
HYPOTHESES
9
PAPERS
0
KG EDGES
473
DEBATES
1

3D Protein Structure

🧬 MAPT — PDB 10KR Click to expand

Experimental structure from RCSB PDB | Powered by Mol*

Druggability & Clinical Context

Druggability
Medium
Score: 0.45
Clinical Stage
Phase III
Target Class
Structural Protein
Safety
0.35
Druggability Analysis
Drug Development0.65
Structural Tractability0.95
Target Class0.50
Safety Profile0.35
Key Metrics
PDB Structures:
134
Known Drugs:
4
Approved:
0
In Clinical Trials:
4
Drug Pipeline (4 compounds)
1 Phase III · 3 Phase II
Druggability Rationale: MAPT demonstrates medium druggability (0.65) with multiple clinical candidates in Phase 2/3 trials, supported by 134 PDB structures and AlphaFold models enabling structure-based design. However, as a structural protein lacking a traditional catalytic pocket, it is best targeted through antibody-based approaches, aggregation inhibitors, and indirect modulation rather than small-molecule active site binders, which explains the moderate druggability score despite robust structural information.
Mechanism: Tau aggregation inhibitors, anti-tau antibodies, tau phosphorylation modulators
Drug Pipeline (4 compounds)
1 Phase III · 3 Phase II
Known Drugs:
LMTX (TRx0237) (phase_3) — Alzheimer's disease
Semorinemab (phase_2) — Alzheimer's disease
Tilavonemab (phase_2) — PSP
Bepranemab (phase_2) — Alzheimer's disease
Structural Data:
PDB (134) ✓AlphaFold ✓Cryo-EM —
10KR1I8H22JY2ON93OVL+129 more
UniProt: A0A7I2PJZ2

Selectivity & Safety Considerations

A major challenge is achieving selectivity between tau isoforms (3R vs 4R tau), as different tauopathies preferentially aggregate specific isoforms; antibody-based therapies can achieve epitope selectivity but small-molecule aggregation inhibitors may lack isoform discrimination. Off-target phosphorylation modulation is a concern, as kinase inhibitors targeting tau phosphorylation regulators may affect multiple kinase pathways with broader CNS effects.

3D Protein Structure

PDB: Open in RCSB AlphaFold model

Interactive 3D viewer powered by RCSB PDB / Mol*. Use mouse to rotate, scroll to zoom.

Clinical Trials (8)

Relevant trials from ClinicalTrials.gov

Active
1
Completed
4
Total Enrollment
1,772
By Phase
PHASE1: 2 · PHASE2: 5 · Unknown: 1
A Study to Test the Safety and Tolerability of Long-term UCB0107 Administration in Study Participants With Progressive S Active Not Recruiting
PHASE1 NCT04658199 n=19
Progressive Supranuclear Palsy
Interventions: UCB0107 (bepranemab)
Sponsor: UCB Biopharma SRL | Started: 2020-11-16
A Study of Semorinemab in Patients With Moderate Alzheimer's Disease Completed
PHASE2 NCT03828747 n=272
Alzheimer's Disease
Interventions: Semorinemab, Placebo, [18F]GTP1
Sponsor: Genentech, Inc. | Started: 2019-01-25
A Study to Test the Efficacy, Safety, and Tolerability of Bepranemab (UCB0107) in Patients With Mild Cognitive Impairmen Completed
PHASE2 NCT04867616 n=466
Alzheimer's Disease
Interventions: Placebo, Bepranemab
Sponsor: UCB Biopharma SRL | Started: 2021-06-09
A Study to Test the Safety and Tolerability of UCB0107 in Study Participants With Progressive Supranuclear Palsy (PSP) Completed
PHASE1 NCT04185415 n=25
Progressive Supranuclear Palsy
Interventions: bepranemab, Placebo
Sponsor: UCB Biopharma SRL | Started: 2019-12-03
Human CNS Tau Kinetics in Tauopathies Completed
Unknown NCT03545126 n=27
Progressive Supranuclear Palsy (PSP), Corticobasal Degeneration (CBD), Frontotemporal Dementia (FTD MAPT Mutati
Interventions: 13C6 Leucine
Sponsor: Washington University School of Medicine | Started: 2017-08-21
A Study to Evaluate the Efficacy and Safety of Semorinemab in Patients With Prodromal to Mild Alzheimer's Disease Terminated
PHASE2 NCT03289143 n=457
Alzheimer's Disease
Interventions: Semorinemab, Placebo, [18F]GTP1
Sponsor: Genentech, Inc. | Started: 2017-10-04
An Extension Study of ABBV-8E12 in Progressive Supranuclear Palsy (PSP) Terminated
PHASE2 NCT03391765 n=142
Progressive Supranuclear Palsy (PSP)
Interventions: ABBV-8E12, Placebo solution for IV infusion on Day
Sponsor: AbbVie | Started: 2018-01-24
An Extension Study of ABBV-8E12 in Early Alzheimer's Disease (AD) Terminated
PHASE2 NCT03712787 n=364
Alzheimer's Disease
Interventions: Tilavonemab
Sponsor: AbbVie | Started: 2019-03-22

Linked Hypotheses (10)

Glymphatic-Mediated Tau Clearance Dysfunction0.821
Excitatory Neuron Synaptic Dysfunction and Mitochondrial Stress via MAPT (tau)0.790
Dual-Circuit Tau Vulnerability Cascade0.754
Cholinergic Basal Forebrain-Hippocampal Circuit Protection0.742
Tau missorting transitions into an autonomous tau-seeding state after transient Aβ exposure0.740
Dopaminergic Ventral Tegmental-Hippocampal Circuit Protection0.740
Microglial-Mediated Tau Clearance Dysfunction via TREM2 Receptor Impairment0.737
Microglial Exosome-Mediated Tau Propagation0.702
Dual-Circuit Tau Vulnerability Cascade with Glial-Mediated Amplification0.696
Microglial TREM2-Mediated Tau Phagocytosis Impairment0.676

Linked Experiments (3)

Microtubule domain analysis in adult axons0.800
Tau depletion effects on microtubule domains in adult axons0.800
Pre-Symptomatic Tau Detection in MAPT Mutation Carriers0.400

Scoring Dimensions

Portfolio 0.36 (25%) Druggability 0.45 (20%) Evidence 0.66 (20%) Safety 0.35 (15%) Competitive 0.00 (10%) Connectivity 0.00 (10%) 0.365 composite

Knowledge Graph (20)

activates (3)

APOEMAPTSREBF1MAPTPSEN2MAPT

associated with (1)

MAPTMAP6

encodes (1)

MAPTTAU

interacts with (15)

NCSTNMAPTFASMAPTTNFMAPTLMNAMAPTAPH1BMAPT
▸ Show 10 more
IL6MAPTA2MMAPTDHCR24MAPTHMGCRMAPTMAPTPARP1MAPTPEN2MAPTPSEN1MAPTDAPK1MAPTHSPG2MAPTIL1B

Debate History (1)

Should MAPT (None) be prioritized as a therapeutic target for neurodegeneration?2026-04-22