Surufatinib is a synthetic small-molecule kinase inhibitor developed as an antineoplastic and anti-angiogenic active pharmaceutical ingredient. It is also known by the development code HMPL-012 and the earlier name sulfatinib. The compound is an orally active inhibitor of several receptor tyrosine kinases involved in tumor angiogenesis and tumor progression. FDA substance records identify Surufatinib with the molecular formula C24H28N6O3S and molecular weight 480.58 g/mol.
Surufatinib has been approved in China and is associated with the treatment of neuroendocrine tumors. IUPHAR/BPS records its China NMPA approval in 2020 and identifies the compound as an orally active synthetic organic drug.
Surufatinib has the chemical name N-[2-(dimethylamino)ethyl]-1-[3-[[4-[(2-methyl-1H-indol-5-yl)oxy]pyrimidin-2-yl]amino]phenyl]methanesulfonamide. Its CAS Registry Number is 1308672-74-3, and FDA GSRS identifies the substance with UNII B2K5L1L8S9. The FDA substance record indicates that Surufatinib is achiral, with no defined stereocenters or optical activity.
Surufatinib acts primarily by inhibiting receptor tyrosine kinases involved in angiogenesis and tumor signaling. Its pharmacological profile includes inhibition of VEGFR1, VEGFR2, VEGFR3 and FGFR1, while published pharmacological resources also identify activity against CSF1R. By interfering with these signaling pathways, Surufatinib can reduce angiogenic signaling and influence tumor-cell proliferation and the tumor microenvironment.
Surufatinib is an oncology-focused API associated particularly with advanced neuroendocrine tumors (NETs). Its multi-target kinase activity makes it relevant to pharmaceutical research and development involving tumor angiogenesis, vascular endothelial growth factor signaling and fibroblast growth factor signaling.
FDA records show that Surufatinib received an orphan-drug designation for pancreatic neuroendocrine tumors, although the U.S. orphan designation was subsequently withdrawn/revoked and the product is not FDA-approved for that indication.
Surufatinib has a molecular formula of C24H28N6O3S and molecular weight of approximately 480.58 g/mol. FDA and PubChem records identify it as an achiral neutral molecule.
Clinical-development documentation describes the active ingredient as a white to off-white powder, insoluble in water and slightly soluble in methyl alcohol or ethyl alcohol. The same source reports a melting-point range of 162–170°C. These values are physical/reference characteristics and should not automatically be treated as pharmacopoeial release specifications.
Surufatinib is manufactured through a multi-step chemical synthesis. An EMA assessment report describes a six-step manufacturing process, consisting of five chemical transformation steps followed by a milling/micronisation operation. The report also states that manufacturing controls, impurity fate/purge studies and in-process acceptance criteria were evaluated as part of the active-substance manufacturing package.
A controlled manufacturing process is important for managing reaction-related impurities, residual solvents, polymorphic/solid-state characteristics and final particle properties.
Quality control of Surufatinib API should include validated identification and assay methods together with appropriate controls for organic impurities, residual solvents, water content, elemental impurities and solid-state properties.
No current universal USP, BP or Ph. Eur. numerical API release specification for Surufatinib was verified in the authoritative sources reviewed. Therefore, numerical release limits should be established against the applicable registered API specification rather than being invented from secondary supplier data.
Surufatinib API should be packed in suitable pharmaceutical-grade, well-closed containers that protect the material from environmental exposure. Storage conditions should follow the manufacturer's validated stability data and applicable regulatory specification.
A pharmaceutical Surufatinib API supply package may include a Certificate of Analysis (CoA), analytical test methods, specification sheet, safety documentation, batch information and other quality/regulatory documents applicable to the intended market.
A qualified Surufatinib API manufacturer in India should maintain controlled synthesis, validated analytical testing, traceable raw materials, impurity-control strategies and appropriate pharmaceutical quality systems. For an oncology API such as Surufatinib, consistent control of assay, related substances, residual solvents, water and physical characteristics is particularly important for reliable downstream pharmaceutical manufacturing.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Melting Point | 162–170°C |