larotrectinib
Trade name: vitrakvi
Small moleculeapprovedOrphan Drug FDABreakthrough Therapy FDA
Approved
Nov 26, 2018
Larotrectinib (previously known as ARRY-470 and LOXO-101) is a potent, oral and selective investigational new drug in clinical development for the treatment of patients with cancers that harbor abnormalities involving the tropomyosin receptor kinases (TRKs). Larotrectinib is in phase II clinical trials for the treatment patients with solid tumors, non-Hodgkin lymphoma and for the pediatric patients with advanced solid or primary CNS tumors. — NCATS
Clinical trial activity
16 trials · 25 clinical orgs · 2 marketing orgs
Phase 1
3
Phase 2
11
Phase 3
0
Phase 4
2
Earliest trial started Apr 1, 2014 (NCT02122913)
Timeline
2010s
- Jan 1, 2014
Loxo Oncology — Earliest Phase 1 Sponsor(trial)
- Jan 1, 2015
Earliest Phase 2 Sponsor(trial)
- May 9, 2017
Orphan Drug Designation
- Nov 26, 2018
Loxo Oncology — Earliest FDA Approval
- Nov 26, 2018
Bayer — NDA Secondary Org
- Nov 26, 2018
Loxo Oncology — NDA Organization
Indications
Approved for
Studied for
- Bile Duct Neoplasms · Phase 2
- Breast Neoplasms · Phase 2
- Central Nervous System Neoplasms · Phase 2
- Colonic Neoplasms · Phase 2
- Colorectal Neoplasms · Phase 2
- Diffuse Intrinsic Pontine Glioma · Early Phase 1
- Endometrial Neoplasms · Phase 2
- Ependymoma · Phase 2
- Esophageal Neoplasms · Phase 2
- Fibrosarcoma · Phase 2
- Glioma · Phase 2
- Hepatoblastoma · Phase 2
- Histiocytosis, Langerhans-Cell · Phase 2
- Kidney Neoplasms · Phase 2
- Leukemia · Phase 2
- Liver Neoplasms · Phase 2
- Lung Neoplasms · Phase 2
- Lymphoma · Phase 2
- Lymphoma, Non-Hodgkin · Phase 2
- Medulloblastoma · Phase 2
- Melanoma · Phase 2
- Multiple Myeloma · Phase 2
- Mutation · Phase 2
- Neoplasm Metastasis · Phase 2
- Neoplasms · Phase 2
- Neoplasms, Germ Cell and Embryonal · Phase 2
- Neuroblastoma · Phase 2
- Osteosarcoma · Phase 2
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 2
- Prostatic Neoplasms · Phase 2
- Rhabdoid Tumor · Phase 2
- Rhabdomyosarcoma · Phase 2
- Sarcoma · Phase 2
- Sarcoma, Ewing · Phase 2
- Skin Neoplasms · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 2
- Thyroid Neoplasms · Phase 4
- Urinary Bladder Neoplasms · Phase 2
- Uterine Cervical Neoplasms · Phase 2
- Uterine Neoplasms · Phase 2
- Wilms Tumor · Phase 2
Mechanism of action
Approval history
- approvedPriority reviewAcceleratedBreakthroughNov 26, 2018
Chemistry & pharmacology
Loading structure…
SMILES
O=C(Nc1cnn2ccc(N3CCC[C@@H]3c3cc(F)ccc3F)nc12)N1CC[C@H](O)C1- Mol. weight
- 428.44 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
First in class
Sources
- ChEMBLCHEMBL3889654 ↗
- WikipediaLarotrectinib ↗
- NCATSPF9462I9HX ↗
- ChEMBLCHEMBL3989939 ↗
- ChEMBLCHEMBL3545075 ↗
Also known as
- arry-470
- larotrectinib
- larotrectinib
- larotrectinib
- loxo-101
- loxo-101
- loxo-101
- n-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07010393 | Phase 4 | Jul 1, 2025 | Fujian Medical University |
| NCT06563999 | Phase 2 | Dec 1, 2024 | Sun Yat-Sen University |
| NCT05783323 | Phase 2 | Feb 29, 2024 | Bayer, University of Pennsylvania |
| NCT05725200 | Phase 2 | Sep 27, 2022 | University of Oslo |
| NCT06482086 | Phase 2 | Jun 1, 2021 | Sichuan University |
| NCT04879121 | Phase 2 | Apr 20, 2021 | University of Texas at Houston |
| NCT04655404 | Early Phase 1 (Phase 1) | Feb 1, 2021 | Ohio State University |
| NCT06195228 | Phase 4 | Jan 1, 2020 | Anhui College of Traditional Chinese Medicine, Central South University, Changhai Hospital, Chinese Academy of Medical Sciences, Dalian Medical University, Fudan University, Fujian Medical University, Henan Medical University, Huazhong University of Science and Technology, Inner Mongolia Medical University, Jiangsu Cancer Institute & Hospital, Jiao Tong University, Shanxi Medical University, Sun Yat-Sen University, Tianjin Medical University, Zhejiang University |
| NCT03834961 | Phase 2 | May 22, 2019 | National Cancer Institute (NCI) |
| NCT03213704 | Phase 2 | Jul 24, 2017 | National Cancer Institute (NCI) |
| NCT06390852 | Phase 2 | Mar 12, 2017 | ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI) |
| NCT03025360 | N/A | Jan 16, 2017 | Loxo Oncology |
| NCT02637687 | Phase 1/Phase 2 (Phase 2) | Dec 1, 2015 | Loxo Oncology |
| NCT02576431 | Phase 2 | Oct 1, 2015 | Loxo Oncology |
| NCT02465060 | Phase 2 | Aug 12, 2015 | ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI) |
| NCT02122913 | Phase 1 | Apr 1, 2014 | Loxo Oncology |
Showing 16 of 16 trials
Page 1 / 1
Organizations
Research & Development (25)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Loxo Oncology | For profit | 4 | 4 | 3 | 2014 |
| National Cancer Institute (NCI) | Government | 4 | 4 | 1 | 2015 |
| ECOG-ACRIN Cancer Research Group | Academic/Hospital | 2 | 0 | 1 | 2015 |
| Fujian Medical University | Academic/Hospital | 2 | 1 | 1 | 2020 |
| Sun Yat-Sen University | Academic/Hospital | 2 | 1 | 2 | 2020 |
| Anhui College of Traditional Chinese Medicine | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Bayer | For profit | 1 | 0 | 1 | 2024 |
| Central South University | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Changhai Hospital | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Dalian Medical University | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Fudan University | Academic/Hospital | 1 | 1 | 1 | 2020 |
| Henan Medical University | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Huazhong University of Science and Technology | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Inner Mongolia Medical University | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Jiangsu Cancer Institute & Hospital | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Jiao Tong University | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Ohio State University | Academic/Hospital | 1 | 1 | 1 | 2021 |
| Shanxi Medical University | Academic/Hospital | 1 | 0 | 1 | 2020 |
| Sichuan University | Academic/Hospital | 1 | 1 | 1 | 2021 |
25 organizations
Page 1 / 2
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Bayer | For profit | NDA2 | Nov 26, 2018 |
| Bayer | For profit | SYN | Nov 26, 2018 |
| Loxo Oncology | For profit | NDA | Nov 26, 2018 |