Taletrectinib API is a next-generation oral tyrosine kinase inhibitor developed to target ROS1 and ROS1 resistance mutations. It is marketed in the United States as Ibtrozi and was approved by the U.S. FDA on June 11, 2025, for adults with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC).
The approved drug substance is taletrectinib adipate, a salt form of the active molecule. FDA identifies its molecular formula as C₂₃H₂₄FN₅O·C₆H₁₀O₄ and molecular weight as 551.61 g/mol.
Taletrectinib is designed to inhibit ROS1 kinase activity, including activity associated with acquired ROS1 resistance mutations, making it an important targeted oncology API.
Taletrectinib is a small-molecule kinase inhibitor belonging to the targeted anticancer drug class. The active molecule inhibits ROS1, a receptor tyrosine kinase that can become oncogenic when activated by gene rearrangements.
The free-base taletrectinib has the molecular formula C₂₃H₂₄FN₅O, molecular weight 405.5 g/mol, and CAS number 1505514-27-1. FDA-approved taletrectinib drug substance is supplied as the adipate salt, with molecular weight 551.61 g/mol.
| Parameter | Details |
|---|---|
| Generic Name | Taletrectinib |
| API Form | Taletrectinib Adipate |
| Free Base CAS Number | 1505514-27-1 |
| Free Base Formula | C₂₃H₂₄FN₅O |
| Free Base Molecular Weight | 405.5 g/mol |
| Adipate Formula | C₂₃H₂₄FN₅O·C₆H₁₀O₄ |
| Adipate Molecular Weight | 551.61 g/mol |
| Chemical Class | Small-molecule kinase inhibitor |
| Target | ROS1 |
| Additional Kinase Activity | TRKA, TRKB and TRKC |
| Therapeutic Category | Antineoplastic / targeted therapy |
| Development Names | AB-106, DS-6051a |
| FDA Brand | Ibtrozi |
| Chiral Centers | 2 |
The FDA chemical name for the approved adipate drug substance is 3-{4-[(2R)-2-aminopropoxy]phenyl}-N-[(1R)-1-(3-fluorophenyl)ethyl]imidazo[1,2-b]pyridazin-6-amine monoadipate. FDA's label specifically notes the two R-configured chiral centers.
Taletrectinib is used as a targeted anticancer therapy for ROS1-positive non-small cell lung cancer.
The U.S. FDA approved Ibtrozi for adults with locally advanced or metastatic ROS1-positive NSCLC. Patient selection is based on the presence of ROS1 rearrangements.
The recommended FDA dosage is 600 mg orally once daily on an empty stomach, with no food intake for at least two hours before and two hours after administration.
Taletrectinib is a kinase inhibitor that binds to and inhibits ROS1 kinase activity. ROS1 rearrangements can result in constitutive kinase signaling that promotes tumor-cell proliferation and survival.
Taletrectinib also demonstrates activity against ROS1 resistance mutations and has inhibitory activity against the TRK family of kinases.
By inhibiting ROS1-mediated signaling, taletrectinib interferes with oncogenic signaling pathways responsible for the growth and survival of ROS1-driven cancer cells.
Taletrectinib adipate API should be evaluated using validated pharmaceutical analytical methods.
Typical quality-control parameters include:
Because Taletrectinib contains two defined stereocenters, stereochemical purity should be appropriately controlled using a validated chiral analytical procedure.
Taletrectinib adipate API manufacturing involves controlled chemical synthesis of the active pharmaceutical ingredient followed by purification, salt formation and solid-state processing.
Key manufacturing controls can include:
Manufacturing should use validated processes and appropriate pharmaceutical quality systems.
PubChem reports a calculated molecular weight of 405.5 g/mol for free-base taletrectinib and XLogP3-AA of approximately 3.8.
Taletrectinib adipate API should be packaged in suitable pharmaceutical-grade containers that protect the material from moisture, contamination and environmental exposure.
Storage conditions should follow the validated stability data and approved API specification. Finished Ibtrozi capsules are stored at controlled room temperature according to FDA-approved labeling; this finished-product condition should not automatically be treated as the API storage specification.
Documentation for Taletrectinib API may include:
A reliable Taletrectinib API Manufacturer in India should provide consistent quality, validated analytical testing and appropriate control of the active molecule and its adipate salt form.
Key considerations include:
Swapnroop can position Taletrectinib adipate as a specialized oncology API offering supported by pharmaceutical quality controls, analytical characterization and technical documentation.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |