Interleukin-1 (IL-1)

Modality

IL-1α/β are part of a broader family of IL-1 cytokines that induce MyD88-dependent signals through a common IL-1 accessory protein (IL-1RAcP) binding to the IL-1R1 subunit. And the natural antagonists IL-1Ra, sIL-1RAcp, and decoy receptor IL-1R2 regulate IL-1α/β functions.

IL-1 receptor antagonist (IL-1Ra), one important member of the IL-1 family, appears to be primarily an anti-inflammatory cytokine. In 1984, IL-1Ra was originally discovered in the urine, serum, and supernatant of cultured monocytes of patients with leukemia.

Application of IL-1RA

As a recombined unglycosylated human interleukin-1 receptor antagonist (IL-1Ra), Anakinra (Kineret, Amgen Inc.) acts on the IL-1/IL-1R1 signal way to augment tear excretion and normalize mucin layer.

Differing from native human IL-1Ra, anakinra has the added single methionine residue at the N-terminus. The single molecule of anakinra consists of 153 amino acids with a molecular weight of 17.3 kDa. Anakinra is expressed in an engineered Escherichia coli (E. coli). The drug is currently approved by the FDA to treat Rheumatoid Arthritis (RA), Cryopyrin-Associated Periodic Syndromes (CAPS), and Deficiency of Interleukin-1 Receptor Antagonist (DIRA).

Yaohai Bio-Pharma Offers One-Stop CDMO Solution for IL-1RA

IL-1Ra Pipelines

Generic Name	Brand Name/ Alternative Name	Expression System	Indications	Manufacturer	R&D Stage
Anakinra	Kineret, Antril, Interleukin-1 receptor antagonist anakinra, RHIL-1RA	Escherichia coli (E. coli)	Rheumatoid Arthritis (RA), Cryopyrin-Associated Periodic Syndromes (CAPS), Deficiency of Interleukin-1 Receptor Antagonist (DIRA), COVID-19 pneumonia	Amgen	Approval
Isunakinra	EBI-005	Pending update	Severe allergic conjunctivitis	Sesen Bio, Inc.	phase 2
GR007	rhIL-1Ra	E. coli	Toxicity induced by chemotherapy agents	Jiaochen Biological	phase 2
NK-003	FC21-NK cell therapy	Pending update	Chronic myeloid leukemia (CML) on TKI therapy	BetterLife Pharma	phase 2
HL-2351	Fc-fused interleukin (IL)-1 receptor antagonist, rhIL-1Ra-hyFc	Pending update	Rheumatoid Arthritis (RA),	Genexine, Inc.	phase 2

Reference:

[1] Broderick L, Hoffman HM. IL-1 and autoinflammatory disease: biology, pathogenesis and therapeutic targeting. Nat Rev Rheumatol. 2022 Aug;18(8):448-463. doi: 10.1038/s41584-022-00797-1.

All Categories

Interleukin-1 (IL-1)

Modality