MedPath

Larotrectinib

Generic Name
Larotrectinib
Brand Names
Vitrakvi
Drug Type
Small Molecule
Chemical Formula
C21H22F2N6O2
CAS Number
1223403-58-4
Unique Ingredient Identifier
PF9462I9HX

Overview

Larotrectinib is an orally administered tropomyosin receptor kinase (Trk) inhibitor with demonstrated antineoplastic activity. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival. Originally discovered by Array BioPharma, the agent was ultimately licensed to Loxo Oncology in 2013. Larotrectinib is another example of innovative new cancer therapy medications that target key, specific genetic biomarker drivers of cancer rather than particular types of tumors .

Background

Larotrectinib is an orally administered tropomyosin receptor kinase (Trk) inhibitor with demonstrated antineoplastic activity. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival. Originally discovered by Array BioPharma, the agent was ultimately licensed to Loxo Oncology in 2013. Larotrectinib is another example of innovative new cancer therapy medications that target key, specific genetic biomarker drivers of cancer rather than particular types of tumors .

Indication

用于治疗携带NTRK基因融合的局部晚期或转移性实体瘤的成人和儿童患者。包括肺癌、甲状腺癌、黑色素瘤、胃肠癌、结肠癌、软酿肉瘤、唾液腺、婴儿纤维肉瘤、阑尾癌、乳腺癌、胆管癌、胰腺癌等多种疾病。

Associated Conditions

  • NTRK1 Fusion Positive
  • NTRK2 Fusion Positive
  • NTRK3 Fusion Positive

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/06/08
Phase 4
Not yet recruiting
Fujian Medical University
2024/08/21
Phase 2
Recruiting
Sun Yat-sen University
2024/07/01
Phase 2
Recruiting
2024/04/30
Phase 2
Active, not recruiting
2023/03/24
Phase 2
Recruiting
2023/02/13
Phase 2
Recruiting
Oslo University Hospital
2022/02/11
N/A
Completed
2021/06/30
N/A
Recruiting
2021/05/10
Phase 2
Recruiting
2020/12/07
Early Phase 1
Recruiting

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Loxo Oncology, Inc.
71777-391
ORAL
100 mg in 1 1
12/5/2018
Bayer HealthCare Pharmaceuticals Inc.
50419-392
OROPHARYNGEAL
20 mg in 1 mL
12/6/2022
Loxo Oncology, Inc.
71777-390
ORAL
25 mg in 1 1
12/5/2018
Bayer HealthCare Pharmaceuticals Inc.
50419-390
ORAL
25 mg in 1 1
12/6/2022
Bayer HealthCare Pharmaceuticals Inc.
50419-393
OROPHARYNGEAL
20 mg in 1 mL
12/6/2022
Bayer HealthCare Pharmaceuticals Inc.
50419-391
ORAL
100 mg in 1 1
12/6/2022
Loxo Oncology, Inc.
71777-392
ORAL
20 mg in 1 mL
12/5/2018

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
Authorised
9/19/2019
Authorised
9/19/2019

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
Larotrectinib Sulfate Capsules
国药准字HJ20220033
化学药品
胶囊剂
4/8/2022
Larotrectinib Sulfate Capsules
国药准字HJ20220032
化学药品
胶囊剂
4/8/2022
Larotrectinib Sulfate Oral Solution
国药准字HJ20220056
化学药品
口服溶液剂
6/23/2022

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

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