Vandetanib is a synthetic small-molecule anticancer active pharmaceutical ingredient (API) belonging to the quinazoline class of tyrosine kinase inhibitors. It is used in pharmaceutical formulations for the treatment of certain forms of medullary thyroid cancer. Vandetanib is also known by the development code ZD6474 and the brand name Caprelsa.
Vandetanib has the chemical formula C22H24BrFN4O2, molecular weight 475.40 g/mol, and CAS Number 443913-73-3. PubChem identifies Vandetanib as a quinazoline derivative containing bromine and fluorine substituents and a methylpiperidine-containing methoxy group.
Vandetanib is chemically named N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine. It is a non-chiral molecule with no defined stereocenters. Its molecular structure contains a quinazoline nucleus, a bromofluorophenyl group, methoxy functionality and a substituted piperidine ring.
The principal product characteristics are:
Vandetanib is a kinase inhibitor that inhibits several receptor tyrosine kinases, including vascular endothelial growth factor receptors (VEGFR), epidermal growth factor receptor (EGFR) and RET. Its inhibition of these signaling pathways is relevant to tumor-cell proliferation and angiogenesis.
Vandetanib was approved by the U.S. FDA in 2011 for adults with unresectable, locally advanced or metastatic medullary thyroid cancer.
Vandetanib is a relatively lipophilic compound, with a reported logP around 5.0. Its aqueous solubility is low; PubChem reports approximately 0.008 mg/mL at 25°C, while other reported measurements indicate substantially higher apparent solubility under certain pH conditions.
A reported melting range for Vandetanib is approximately 234–243°C. This value is useful as a physical characterization reference but should not automatically be entered as a pharmacopoeial release specification unless it forms part of the manufacturer's approved specification.
Vandetanib is a synthetic small-molecule API and can be controlled using conventional pharmaceutical analytical techniques such as HPLC, infrared spectroscopy, chromatographic impurity profiling, water determination and residue-on-ignition testing where applicable.
I could not verify a current USP or Ph. Eur. monograph providing universal numerical release limits for Vandetanib. Therefore, numerical values such as 98–102% assay, 0.5% LOD, or 0.1% residue on ignition should not be presented as official compendial requirements without a supporting approved specification.
For a commercial Vandetanib API, the final acceptance criteria should be based on the applicable regulatory filing, customer specification and validated manufacturer's specification.
Swapnroop Drugs & Pharmaceuticals provides pharmaceutical API sourcing and supply support for Vandetanib API for pharmaceutical development and manufacturing applications.
As a Vandetanib API manufacturer and supplier in India, the product can be positioned for pharmaceutical companies requiring an oncology API with controlled chemical identity, assay, related substances, residual solvents and other applicable quality attributes.
Typical documentation may include:
Vandetanib API should be stored in suitable pharmaceutical packaging under controlled conditions established by the applicable product specification and stability data. Published information indicates that solid Vandetanib is relatively stable to thermal and hydrolytic degradation, while degradation can occur under certain photolytic and solution stress conditions.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Melting Point | 234–243°C |