mobocertinib
Trade name: EXKIVITY
Small moleculeapprovedOrphan Drug FDAFast Track FDABreakthrough Therapy FDA
Approved
Sep 15, 2021
Clinical trial activity
11 trials · 2 clinical orgs · 1 marketing orgs
Phase 1
8
Phase 2
2
Phase 3
1
Phase 4
0
Earliest trial started Mar 28, 2018 (NCT03482453)
Timeline
2010s
Indications
Approved for
Mechanism of action
- Epidermal growth factor receptorANTAGONIST
Epidermal growth factor receptor antagonist
Epidermal growth factor receptor erbB1 inhibitor
Inhibits EGFR exon 20 insertion mutants at lower concentrations than wild type. Also inhibits HER2, HER4 and BLK kinases.
Approval history
- approvedPriority reviewAcceleratedFast trackBreakthroughSep 15, 2021
Chemistry & pharmacology
Loading structure…
SMILES
C=CC(=O)Nc1cc(Nc2ncc(C(=O)OC(C)C)c(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C- Mol. weight
- 585.71 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Black box warning
Sources
- ChEMBLCHEMBL4802239 ↗
- ChEMBLCHEMBL4650319 ↗
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04576208 | Phase 2 | Nov 30, 2020 | Takeda |
| NCT04441255 | Phase 1 | Jul 1, 2020 | Takeda |
| NCT04129502 | Phase 3 | Oct 15, 2019 | Millennium Pharmaceuticals |
| NCT04051827 | Phase 1 | Sep 28, 2019 | Millennium Pharmaceuticals |
| NCT04056455 | Phase 1 | Aug 22, 2019 | Millennium Pharmaceuticals |
| NCT04056468 | Phase 1 | Aug 20, 2019 | Millennium Pharmaceuticals |
| NCT03928327 | Phase 1 | May 2, 2019 | Millennium Pharmaceuticals |
| NCT03807778 | Phase 1 | Feb 4, 2019 | Takeda |
| NCT03811834 | Phase 1 | Jan 22, 2019 | Millennium Pharmaceuticals |
| NCT03482453 | Phase 1 | Mar 28, 2018 | Millennium Pharmaceuticals |
| NCT04535557 | N/A | — | Millennium Pharmaceuticals |
Showing 11 of 11 trials
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Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Millennium Pharmaceuticals | For profit | 8 | 8 | 3 | 2018 |
| Takeda | For profit | 3 | 3 | 2 | 2019 |
2 organizations
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