Oprelvekin

Identification

Summary

Oprelvekin is a form of recombinant interleukin-11 used to stimulate production of megakaryocytes and platelets in patients with or at risk of thrombocytopenia after chemotherapy.

Generic Name

Oprelvekin

DrugBank Accession Number

DB00038

Background

Oprelvekin, the active ingredient in Neumega®, is recombinant Interleukin-11 (IL-11), which is produced in Escherichia coli (E. coli) by recombinant DNA technology. With a molecular mass of approximately 19,000 daltons, the non-glycosylated protein is 177 amino acids in length in comparison to the natural IL-11, which is 178 amino acid long. However, it displays comparable biological activity compared to the natural IL-11 in vitro and in vivo. Oprelvekin works by stimulating megakaryocytopoiesis and thrombopoiesis. In mice and nonhuman primate studies of animals with moderate and severe myelosuppression, in addition to compromised hematopoiesis, oprelvekin was shown to potently induce thrombopoiesis and improve platelet nadirs and accelerated platelet recoveries compared to controls. In animal studies, oprelvekin was also shown to regulate intestinal epithelium growth by enhancing healing of gastrointestinal lesions, inhibit adiopegenesis and macrophageal released pro-inflammatory cytokines, and induce acute phase protein synthesis.

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Interleukin-based products

Protein Structure

Protein Chemical Formula: C₈₅₄H₁₄₁₁N₂₅₃O₂₃₅S₂
Protein Average Weight: 19047.2 Da

Sequences

>DB00038 sequence
GPPPGPPRVSPDPRAELDSTVLLTRSLLADTRQLAAQLRDKFPADGDHNLDSLPTLAMSA
GALGALQLPGVLTRLRADLLSYLRHVQWLRRAGGSSLKTLEPELGTLQARLDRLLRRLQL
LMSRLALPQPPPDPPAPPLAPPSSAWGGIRAAHAILGGLHLTLDWAVRGLLLLKTRL

Download FASTA Format

Synonyms

IL-11
Interleukin 11
Interleukin-11
Oprelvekin
Recombinant interleukin-11

External IDs

YM 294

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Pharmacology

Indication

Indicated for the prevention of severe thrombocytopenia and the reduction of the need for platelet transfusions following myelosuppressive chemotherapy in adult patients with nonmyeloid malignancies who are at high risk of severe thrombocytopenia.[Label]

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Prophylaxis of	Severe thrombocytopenia		••••••••••••	•••••	••••••••••• ••••••••••••• ••••••••• •• •••••••• •••••	•••••••••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Oprelvekin promotes hematopoiesis by stimulating megakaryocytopoiesis and thrombopoiesis. It is used in adult patients with nonmyeloid malignancies to prevent severe thrombocytopenia and reduce the need for platelet transfusions following therapies that cause myelosuppression. Its use is prioritized in patients who are at an elevated risk for developing severe thrombocytopenia. In clinical trials, oprelvekin has shown potent thrombopoietic activity in individuals with compromised hematopoiesis.

Mechanism of action

Oprelvekin binds to the interleukin 11 receptor which leads to a cascade of signal transduction events. Its pharmacological action mimics the biological activity of endogenous IL-11, which is a thrombopoietic growth factor that directly stimulates the proliferation of hematopoietic stem cells and megakaryocyte progenitor cells and induces megakaryocyte maturation resulting in increased platelet production.

Target	Actions	Organism
AInterleukin-11 receptor subunit alpha	agonist	Humans

Absorption

Absolute bioavailability is over 80%.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

The kidney is the primary route of elimination. The amount of intact Neumega in urine was low, indicating that the molecule was metabolized before excretion.

Half-life

6.9 +/- 1.7 hrs

Clearance

Not Available

Adverse Effects

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Toxicity

Not Available

Pathways

Not Available

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">: This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions: Not Available

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Neumega	Kit	5 mg/1mL	Subcutaneous	Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.	1997-11-01	2017-04-30

Chemical Identifiers

UNII: HM5641GA6F
CAS number: 145941-26-0

References

General References

Not Available

External Links

UniProt: P20809
Genbank: M57765
PubChem Substance: 46506470
RxNav: 1311380
ChEMBL: CHEMBL1201573
Therapeutic Targets Database: DAP001287
PharmGKB: PA164747991
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Oprelvekin

FDA label

Download (57.8 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Pancytopenia Due to Chemotherapy	1
3	Completed	Prevention	Chemotherapy-Induced Thrombocytopenia	1
3	Unknown Status	Treatment	Nasopharyngeal Carcinoma (NPC)	1
2	Completed	Prevention	Von Willebrand's Disease	1
2	Completed	Treatment	Breast Cancer / Gestational Trophoblastic Neoplasia / Lymphoma / Neuroblastoma (NB) / Ovarian Cancer / Renal Cancer / Sarcomas / Testicular germ cell tumour	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Physicians Total Care Inc.
Wyeth Pharmaceuticals

Dosage Forms

Form	Route	Strength
Kit	Subcutaneous	5 mg/1mL

Prices

Unit description	Cost	Unit
Neumega 5 mg vial	352.9USD	vial

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Not Available

Properties

State

Liquid

Experimental Properties

Property	Value	Source
hydrophobicity	-0.070	Not Available
isoelectric point	11.16	Not Available

Targets

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Details1. Interleukin-11 receptor subunit alpha

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

General Function: Transmembrane signaling receptor activity
Specific Function: Receptor for interleukin-11. The receptor systems for IL6, LIF, OSM, CNTF, IL11 and CT1 can utilize IL6ST for initiating signal transmission. The IL11/IL11RA/IL6ST complex may be involved in the co...
Gene Name: IL11RA
Uniprot ID: Q14626
Uniprot Name: Interleukin-11 receptor subunit alpha
Molecular Weight: 45221.925 Da

References

Nandurkar HH, Robb L, Begley CG: The role of IL-II in hematopoiesis as revealed by a targeted mutation of its receptor. Stem Cells. 1998;16 Suppl 2:53-65. [Article]
Li R, Hartley L, Robb L: Cloning of rat interleukin 11 and interleukin 11 receptor alpha chain and analysis of their expression in rat uterus in the peri-implantation period. Reproduction. 2001 Oct;122(4):593-600. [Article]
Nandurkar HH, Hilton DJ, Nathan P, Willson T, Nicola N, Begley CG: The human IL-11 receptor requires gp130 for signalling: demonstration by molecular cloning of the receptor. Oncogene. 1996 Feb 1;12(3):585-93. [Article]
Romas E, Udagawa N, Zhou H, Tamura T, Saito M, Taga T, Hilton DJ, Suda T, Ng KW, Martin TJ: The role of gp130-mediated signals in osteoclast development: regulation of interleukin 11 production by osteoblasts and distribution of its receptor in bone marrow cultures. J Exp Med. 1996 Jun 1;183(6):2581-91. [Article]
Nandurkar HH, Robb L, Tarlinton D, Barnett L, Kontgen F, Begley CG: Adult mice with targeted mutation of the interleukin-11 receptor (IL11Ra) display normal hematopoiesis. Blood. 1997 Sep 15;90(6):2148-59. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Drug created at June 13, 2005 13:24 / Updated at January 02, 2024 23:41

Oprelvekin

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References