Table 1.

Characteristics and specifications for clinical grade rintatolimod.

Generic name: Rintatolimod

Brand name: Ampligen

Molecular Formula

Poly I: Poly C12U is designated by the molecular formula, [rI(13):rC(12)rU(1)]n where: n = 46–138, or (C10 H11 N4 O7 P)13: (C9 H12 N3 O7 P)12 (C9 H11 N2 O8 P).

Molecular Weight

400,000–1,200,000 (10.0–15.0 S20w)

Chemical Abstracts (CAS) Registry Number

38640–92-5

Chemical Name

• Chemical abstracts names: 5ʹ-Inosinic acid, homopolymer, complex with 5ʹ-cytidylic acid polymer with 5ʹ-uridylic acid (1:1) (9CI) (CA INDEX NAME) 5ʹ-Cytidylic acid, polymer with 5ʹ-uridylic acid, complex with 5ʹ-inosinic acid homopolymer (1:1) (9CI) 5ʹ-Uridylic acid, polymer with 5ʹ-cytidylic acid, complex with 5ʹ-inosinic acid homopolymer (1:1) (9CI) Ampligen Poly(I).poly(C12U)

• Other names: Polyriboinosinic-polyribocytidylic 12: uridylic acid; Poly I: Poly C12U Rintatolimod

Nucleotide composition

The ratio of poly I to poly C12U is 0.9–1.1–1.0

Formulation

Rintatolimod is supplied in glass bottles as a biological active (TLR3 agonist in Ramos-BlueTM reporter cells), sterile, colorless solution containing 200 mg of Poly I: Poly C12U in 80 ml of a physiological solution of salts (0.15 M NaCl, 0.01 M Phosphate, 0.001 Mg++) at a concentration of 2.5 mg/ml (2.25–2.70 mg/ml) with tertiary conformation demonstrated by circular dichroism. The product does not contain preservatives or antioxidants and is free of particulates (Particles ≥10 µm < 3000 per container; Particles ≥25 µm < 300 per container) and endotoxins (LAL activity < 1 EU/mL). The shelf life at 2–8°C is >7 years.