Data updated: May 26, 2026
TUKYSA (tucatinib)
Tyrosine Kinase Inhibitors Genetically Validated
Trial Activity: Growth 28 active trials
Orphan Drug Breakthrough Therapy Priority Review Fast Track
Oncology
Approved 2020-04-17
TUKYSA is indicated for the treatment of Breast Cancer; Colorectal Cancer.
How TUKYSA Works
Tucatinib is a tyrosine kinase inhibitor of HER2. In vitro, tucatinib inhibits the phosphorylation of HER2 and HER3, resulting in the inhibition of downstream MAPK and AKT signaling and cell proliferation. It has demonstrated anti-tumor activity in HER2-expressing tumor cells in both in vitro and in vivo settings. The combination of tucatinib and trastuzumab has shown increased anti-tumor activity compared to either drug used alone.
Development Insights
Seagen Inc. conducting 9 trials (17%)
120 indications explored (Broad Platform)
→ breast cancer (11 trials)
→ her2-positive breast cancer (8 trials)
→ metastatic breast cancer (6 trials)
2
Indications
--
Phase 3 Trials
2
Priority Reviews
6
Years on Market
Details
- Status
- Prescription
- First Approved
- 2020-04-17
- Patent Cliff
- 2038
- Routes
- ORAL
- Dosage Forms
- TABLET
TUKYSA Approval History
2021
2022
2023
2024
2025
2026
Original
New Indication
New Form
Label Update
4 FDA actions from 2020 to 2023 · 1 indication expansions
What TUKYSA Treats
2 indicationsTUKYSA is approved for 2 conditions since its original approval in 2020. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Breast Cancer
- Colorectal Cancer
Source: FDA Label
TUKYSA Target & Pathway
ProTarget
A receptor tyrosine kinase that promotes cell growth and division. Approximately 20% of breast cancers overexpress HER2, leading to aggressive tumor growth. Targeting HER2 blocks these growth signals and can trigger immune-mediated destruction of cancer cells.
Pathway Context
HER2 forms dimers with other HER family members to activate growth signaling
HER3 (Human Epidermal Growth Factor Receptor 3)
EGFR (Epidermal Growth Factor Receptor) receptor
A receptor that triggers cell growth, proliferation, and survival when activated. Mutations or overexpression of EGFR drive many cancers, particularly lung cancer. Blocking EGFR stops the growth signals that fuel tumor progression.
TUKYSA Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Direct competitors
10
Same target(s) AND same indication — head-to-head.
MoA expansion candidates
7
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
10
Same indication, different mechanism — what else might this patient receive?
Unlock 21 more competitors across all three rings.
Upgrade to Pro Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in TUKYSA's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications TUKYSA treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to TUKYSA
3 of 20FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
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Clinical Trial Registry
51 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT05672524 | 22-185 | Ph 2 | recruiting | A Study of Tucatinib and Trastuzumab in People With Rectal Cancer |
| NCT07413939 BREnnA | WO46069 2025-524498-17-00 | Ph 2, Ph 3 | recruiting | RO7771950 Versus Tucatinib in Combination With Trastuzumab and Capecitabine in People With Locally Advanced or Metastatic Breast Cancer That is Human Epidermal Growth Factor Receptor 2 (HER2)-Positive |
| NCT05319873 | 21-001819 NCI-2021-11707 | Ph 1, Ph 2 | active not recruiting | Ribociclib, Tucatinib, and Trastuzumab for the Treatment of HER2 Positive Breast Cancer |
| NCT06157892 | SGNDV-004 C5731004, 2023-507555-29-00 | Ph 2 | recruiting | A Study of Disitamab Vedotin With Other Anticancer Drugs in Solid Tumors |
| NCT07494448 JAZMINE | MEDOPP0776 2025-524613-89-00 | Ph 1, Ph 2 | not yet recruiting | Phase Ib/II Study of Zanidatamab Plus Tucatinib and Chemotherapy in HER2-Positive Advanced Breast Cancer |
| NCT05132582 HER2CLIMB-05 | SGNTUC-028 C4251007, 2023-503826-37-00 | Ph 3 | active not recruiting | A Study of Tucatinib or Placebo With Trastuzumab and Pertuzumab for Metastatic HER2+ Breast Cancer |
| NCT05253651 MOUNTAINEER-03 | SGNTUC-029 C4251008, 2024-514180-25-00 | Ph 3 | recruiting | A Study of Tucatinib With Trastuzumab and mFOLFOX6 Versus Standard of Care Treatment in First-line HER2+ Metastatic Colorectal Cancer |
| NCT05458674 | 02AB21-TucErBit | Ph 2 | recruiting | Tucatinib+Trastuzumab+Eribulin in HER2+ MBC |
| NCT03975647 results posted | SGNTUC-016 C4251001, 2024-514733-38-00 | Ph 3 | active not recruiting | A Study of Tucatinib vs. Placebo in Combination With Ado-trastuzumab Emtansine (T-DM1) for Patients With Advanced or Metastatic HER2+ Breast Cancer |
| NCT03297606 CAPTUR | PM1 ESR-17-12831, CA209-9DL | Ph 2 | recruiting | Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) |
| NCT04539938 HER2CLIMB-04 results posted | SGNTUC-025 C4251006 | Ph 2 | completed | A Study of Tucatinib Plus Trastuzumab Deruxtecan in HER2+ Breast Cancer |
| NCT05748834 | BRE 381 | Ph 2 | recruiting | Study of Tucatinib and Doxil in Participants With Human Epidermal Growth Factor Receptor 2 Positive (HER2+) Metastatic Breast Cancer |
| NCT05323955 BRIDGET | Pro00109777 | Ph 2 | active not recruiting | Secondary BRain Metastases Prevention After Isolated Intracranial Progression on Trastuzumab/Pertuzumab or T-DM1 in Patients With aDvanced Human Epidermal Growth Factor Receptor 2+ brEast Cancer With the Addition of Tucatinib |
| NCT05230810 | 01AB21- PIK3CA | Ph 1, Ph 2 | active not recruiting | Clinical Trial of Alpelisb and Tucatinib in Patients With PIK3CA-Mutant HER2+ Metastatic Breast Cancer. |
| NCT05382364 | MK-7119-002 C4251016, 7119-002 | Ph 1 | active not recruiting | Safety and Pharmacokinetics of Tucatinib (MK-7119) in Chinese Participants With Cancer (MK-7119-002) |
| NCT04430738 results posted | SGNTUC-024 C4251005 | Ph 2 | active not recruiting | Tucatinib Plus Trastuzumab and Oxaliplatin-based Chemotherapy or Pembrolizumab-containing Combinations for HER2+ Gastrointestinal Cancers |
| NCT05892068 | 22-168 | Ph 2 | active not recruiting | A Study of Tucatinib Given Before Surgery to People With HER2+ Cancers That Have Spread to the Brain |
| NCT06686394 | 1022-009 MK-1022-009, jRCT2041250022 | Ph 1, Ph 2 | recruiting | Study of Patritumab Deruxtecan With Other Anticancer Agents in Participants With HER2 Positive Breast Cancer That Has Spread and Cannot Be Surgically Removed (MK-1022-009) |
| NCT05062889 ERASE-CRC | ERASE-CRC | Ph 2 | suspended | Exploiting Circulating Tumour DNA to Intensify the Postoperative Treatment Resected Colon Cancer Patients |
| NCT05673928 | 2021-0899 NCI-2022-11157 | Ph 2 | recruiting | A Phase II Study of Tucatinib and Ado-trastuzumab Emtansine (T-DM1) in Patients With HER2-positive Metastatic Solid Tumors and Metastases to Brain (TUCATEMEB) |
| NCT04721977 results posted | 7119-001 MK-7119-001, jRCT2051200152 | Ph 2 | active not recruiting | A Study of Tucatinib (MK-7119) in Combination With Trastuzumab and Capecitabine in Participants With Previously Treated Locally Advanced Unresectable or Metastatic Human Epidermal Growth Factor Receptor 2 Positive (HER2+) Breast Carcinoma (MK-7119-001) |
| NCT04579380 results posted | SGNTUC-019 | Ph 2 | active not recruiting | Basket Study of Tucatinib and Trastuzumab in Solid Tumors With HER2 Alterations |
| NCT05583110 TrasTUCAN | GEICAM/2020-08 2021-002561-18 | Ph 2 | terminated | Efficacy and Safety of the Combination of Trastuzumab Plus TUCAtinib Plus viNorelbine in Patients With HER2-positive Non-resectable Locally Advanced or Metastatic Breast Cancer |
| NCT04538742 DB-07 | D967JC00001 2023-505309-18-00, 2019-004531-22 | Ph 1, Ph 2 | active not recruiting | A Phase 1b/2 Study of T-DXd Combinations in HER2-positive Metastatic Breast Cancer |
| NCT05041842 InTTercePT | UC-BCG-2011 2020-005735-79 | Ph 2 | active not recruiting | Treatment With Tucatinib in Patients With an Isolated Brain Progression of a Metastatic Breast Cancer |
| NCT04457596 | A011801 NCI-2020-03770, U10CA180821 | Ph 3 | active not recruiting | T-DM1 and Tucatinib Compared With T-DM1 Alone in Preventing Relapses in People With High Risk HER2-Positive Breast Cancer, the CompassHER2 RD Trial |
| NCT06239467 PIKture-01 | OKI-219-101 | Ph 1 | recruiting | First-in-Human Study of OKI-219 in Advanced Solid Tumors and Advanced Breast Cancer |
| NCT03501979 results posted | UAB 1794 | Ph 2 | terminated | Tucatinib, Trastuzumab, and Capecitabine for the Treatment of HER2+ LMD |
| NCT06439693 | 24-223 TBCRC065 | Ph 2 | recruiting | The SAPPHO Study: Sequential Therapy With Curative Intent in de Novo HER2+ Metastatic Breast Cancer |
| NCT04789096 TUGETHER | BCT 2102 | Ph 2 | terminated | Tucatinib Together With Pembrolizumab and Trastuzumab |
| NCT05868226 PRE-I-SPY-PI | I-SPY-P1 | Ph 1 | recruiting | PRE-I-SPY Phase I/Ib Oncology Platform Program |
| NCT04499924 MOUNTAINEER-02 results posted | SGNTUC-022 C4251004 | Ph 2, Ph 3 | completed | Tucatinib, Trastuzumab, Ramucirumab, and Paclitaxel Versus Paclitaxel and Ramucirumab in Previously Treated HER2+ Gastroesophageal Cancer |
| NCT04632992 MyTACTIC results posted | ML42439 | Ph 2 | completed | A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response |
| NCT02892123 | ZWI-ZW25-101 | Ph 1 | completed | Trial of ZW25 (Zanidatamab) in Patients With Advanced HER2-expressing Cancers |
| NCT03043313 results posted | SGNTUC-017 NCI-2017-01107, ACCRU-GI-1617 | Ph 2 | completed | Tucatinib Plus Trastuzumab in Patients With HER2+ Colorectal Cancer |
| NCT05356897 | ACCRU-GI-2003 NCI-2022-03147, ACCRU-GI-2003 | Ph 2 | withdrawn | Tucatinib Combined with Trastuzumab and TAS-102 for the Treatment of HER2 Positive Metastatic Colorectal Cancer in Molecularly Selected Patients, 3T Study |
| NCT06162559 TRAIN-4 | N21TRV | Ph 1 | recruiting | Neoadjuvant Trastuzumab, Pertuzumab and Tucatinib Without Chemotherapy in HER2-positive Breast Cancer: the TRAIN-4 Study |
| NCT06067776 | UCDCC#298 NCI-2022-04431, UCDCC#298 | Ph 1 | not yet recruiting | Osimertinib, Cetuximab, and Tucatinib for the Treatment of EGFR-Mutant Stage IV or Recurrent Non-small Lung Cell Cancer |
| NCT02614794 HER2CLIMB results posted | ONT-380-206 2015-002801-12 | Ph 2 | completed | A Study of Tucatinib vs. Placebo in Combination With Capecitabine & Trastuzumab in Patients With Advanced HER2+ Breast Cancer |
| NCT04896320 2019-101826 | 2021000247 | Ph 1, Ph 2 | withdrawn | Tucatinib With Chemotherapy and Trastuzumab in Advanced Her-2-neu Overexpressing, Previously Treated Breast Cancer. |
| NCT05091528 results posted | SBT6050-201 | Ph 1, Ph 2 | terminated | A Safety and Activity Study of SBT6050 in Combination With Other HER2-directed Therapies for HER2-positive Cancers |
| NCT05227131 MARGARET | MEDOPP447 2021-006387-24 | Ph 2 | withdrawn | Margetuximab Plus Tucatinib and Capecitabine in HER2-positive Metastatic Breast Cancer |
| NCT04512261 TOPAZ | IIT2019-21-Basho-TOPAZ | Ph 1, Ph 2 | withdrawn | TOPAZ: Tucatinib in COmbination With Pembrolizumab And TrastuZumab in Patients With HER2-Positive Breast Cancer Brain Metastases |
| NCT03846583 | 18-621 | Ph 1 | withdrawn | Tucatinib + Abemaciclib + Herceptin for HER2+ MBC |
| NCT02025192 | ONT-380-005 | Ph 1 | completed | A Study of Tucatinib (ONT-380) Combined With Capecitabine and/or Trastuzumab in Patients With HER2+ Metastatic Breast Cancer |
| NCT03723395 | ONT-380-012 | Ph 1 | completed | A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib |
| NCT03914755 | SGNTUC-015 | Ph 1 | completed | A Safety, Tolerability, and Pharmacokinetic Study of Tucatinib in Healthy Japanese and Caucasian Subjects |
| NCT03722823 | ONT-380-009 | Ph 1 | completed | A Safety Study of Tucatinib in Healthy and Hepatically-Impaired Subjects |
| NCT03777761 | ONT-380-011 | Ph 1 | completed | Effects of Tucatinib on Cardiac Repolarization in Healthy Participants |
| NCT03826602 | SGNTUC-020 | Ph 1 | completed | A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib on Metformin |
Showing 50 of 51 trials
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Pro Active Pipeline
Ongoing clinical trials by development phase
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Pro Key Completed Trials
Completed studies with published results, ranked by significance
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Trial Timeline
Full development history with FDA approval milestones
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Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
TUKYSA FDA Label Details
Indications & Usage
FDA Label (PDF)TUKYSA is indicated for the treatment of Breast Cancer; Colorectal Cancer.
View full patent landscape →
7 OB patents · 4 families ·
255 international docs across 46 countries
TUKYSA Patents & Exclusivity
Latest Patent: Apr 2038
Exclusivity: Jan 2030
Patents (7 active)
US11666572
Expires Apr 27, 2038
US12048698
Expires Apr 27, 2038
US11207324
Expires Apr 27, 2038
US8648087
Expires Apr 17, 2034
US11504370
Expires Mar 25, 2033
US9457093
Expires Oct 12, 2032
US9693989
Expires May 9, 2027
Exclusivity
I-906
Until Jan 2026
ODE-309
Until Apr 2027
ODE-422
Until Jan 2030
I-906
Until Jan 2026
ODE-309
Until Apr 2027
ODE-422
Until Jan 2030
I-906
Until Jan 2026
ODE-309
Until Apr 2027
ODE-422
Until Jan 2030
I-906
Until Jan 2026
ODE-309
Until Apr 2027
ODE-422
Until Jan 2030
Source: FDA Orange Book
Pro Intelligence Preview
Deep insights for TUKYSA
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2038
- • 28 active patents
Trial Analysis
- • 52 total trials
- • Stage: Growth
Competitive Landscape
- • 20 similar drugs
- • Same target/indication analysis
Unlock Full Intelligence
Full approval history • All patents • Revenue trends • Competitor analysis
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment