Nelarabine API Manufacturer in India

Swapnroop Pharma · WHO-GMP Certified · +91 87670 62101

Nelarabine API

Nelarabine is a synthetic purine nucleoside analogue and antineoplastic pharmaceutical API used in oncology. It is a prodrug of 9-β-D-arabinofuranosylguanine (ara-G) and is converted intracellularly to active ara-G nucleotides, ultimately interfering with DNA synthesis.

Nelarabine is primarily associated with pharmaceutical formulations for T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL). Its development code and commonly reported synonym include 506U78 / GW506U78.

Nelarabine API Manufacturer in India

Nelarabine is a well-characterized antineoplastic purine nucleoside analogue API relevant to oncology formulation development, pharmaceutical research, analytical testing and manufacturing applications.

Important API quality attributes include identity, assay, related substances, water content, residual solvents, elemental impurities, optical purity and other applicable pharmaceutical quality parameters.

Chemical Information

CAS Number: 121032-29-9

Molecular Formula: C11H15N5O5

Molecular Weight: 297.27 g/mol

Chemical Name: 9-β-D-Arabinofuranosyl-6-methoxy-9H-purin-2-amine

Development Code: 506U78 / GW506U78

Drug Class: Purine Nucleoside Analogue

Therapeutic Class: Antineoplastic / Antimetabolite

Therapeutic Area: Oncology / Hematology

Molecule Type: Synthetic Small Molecule

The CAS number, molecular formula and molecular weight are consistent across PubChem and chemical-reference sources.

Mechanism of Action

Nelarabine functions as a prodrug of ara-G. Following conversion to active nucleotide metabolites, its pharmacological activity interferes with DNA synthesis.

Its mechanism includes:

  • Conversion to active ara-G metabolites
  • Formation of ara-GTP within cells
  • Interference with DNA synthesis
  • Incorporation of active nucleotide metabolites into DNA
  • Inhibition of DNA elongation
  • Induction of cellular damage and apoptosis
  • Antineoplastic activity against susceptible T-cell malignancies

Nelarabine is particularly relevant to T-cell malignancies, including T-ALL and T-LBL.

Pharmaceutical Applications

Nelarabine API is relevant to:

  • T-cell acute lymphoblastic leukemia formulations
  • T-cell lymphoblastic lymphoma formulations
  • Antineoplastic drug development
  • Purine nucleoside analogue research
  • Oncology pharmaceutical development
  • Antimetabolite research
  • DNA synthesis research
  • Pharmaceutical API manufacturing
  • Analytical and quality-control testing
  • Pharmaceutical research and development

Oncology Applications

Nelarabine is used as an antineoplastic agent in the treatment of T-cell acute lymphoblastic leukemia and T-cell lymphoblastic lymphoma, particularly in specified relapsed or refractory disease settings depending on the applicable regulatory labeling.

Its activity is associated with the intracellular formation of ara-GTP and subsequent disruption of DNA synthesis.

Purine Nucleoside Analogue

Nelarabine belongs to the purine nucleoside analogue class. Structurally, it is a modified guanine nucleoside in which a methoxy group is present on the purine ring.

Its nucleoside structure enables intracellular conversion to active metabolites that interfere with DNA replication, making it relevant to antineoplastic drug development and T-cell malignancy research.

Physical Characteristics

Nelarabine is generally described as a white to off-white powder or solid. Chemical-reference data report a melting range around 209–217°C, while different research-product sources can report differing physical-property measurements.

Nelarabine is reported to have limited aqueous solubility under ordinary conditions, with some sources reporting approximately 5 mg/mL in water when warmed.

Manufacturing Process

A controlled Nelarabine API manufacturing process may involve:

  1. Qualification of starting materials
  2. Preparation of appropriate purine intermediates
  3. Protection of reactive functional groups where required
  4. Glycosylation with an appropriate arabinofuranose intermediate
  5. Controlled introduction of the methoxy substituent
  6. Deprotection
  7. Reaction monitoring
  8. Purification
  9. Crystallization or suitable isolation
  10. Filtration and washing
  11. Controlled drying
  12. Milling, where required
  13. Final analytical testing
  14. GMP-compliant packaging

Quality Control Testing

Typical Nelarabine API testing may include:

  • Identification by IR
  • HPLC identification
  • Assay by HPLC
  • Related substances
  • Degradation products
  • Water content
  • Residual solvents
  • Elemental impurities
  • Optical/chiral purity, where applicable
  • Particle-size distribution, where applicable
  • Stability testing

Detailed Specifications

Parameter Specification
Appearance White crystalline powder or crystals
Identification IR & HPLC compliant
Assay (HPLC) 98.0% – 102.0%
Loss on Drying NMT 1.0%
Residue on Ignition NMT 0.5%
Individual Impurity NMT 0.5%
Total Impurities NMT 2.0%
Water Content NMT 0.5%
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