Olaratumab

Olaratumab Uses, Dosage, Side Effects, Food Interaction and all others data.

Olaratumab (IMC-3G3) is a fully human IgG1 monoclonal antibody with antitumor activity that selectively binds the external domain of human platelet-derived growth factor receptor (PDGFR)-α with high affinity and blocks ligand binding. It is composed of two heavy chain molecule fragments and 2 light chain fragments. Studies show that the treatment of olaratumab in combination with doxorubicin resulted in significant reduction of cancer cell proliferation and tumor growth. Olaratumab was granted accelerated approval (as Lartruvo) as initial therapy to treat adults with certain types of soft tissue sarcoma (STS) in October, 2016.

It exerts an anti-tumor activity in vivo and in vitro against selected sarcoma cells by inhibiting tumor growth by binding to PDGFR-alpha that is present on several types of cancer on transformed cells and in tumor stroma . Olaratumab antibody binding leads to inhibition of ligand-dependent signaling in PDGFR(alpha)-expressing tumor cells, as well as stromal cells in the tumor microenviroment that are dependent on PDGFR(alpha) signaling. When used in a combination therapy with doxorubicin, olaratumab improves progression-free survival in patients with advanced soft-tissue sarcoma.

Trade Name Olaratumab
Availability Discontinued
Generic Olaratumab
Olaratumab Other Names Olaratumab
Related Drugs doxorubicin, Adriamycin, Votrient, pazopanib, Yondelis
Type Intravenous
Formula C6554H10076N1736O2048S40
Weight 154000.0 Da (147200 Da without glycan mass/154600 Da with glycan mass)
Protein binding

None

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Olaratumab
Olaratumab

Uses

Olaratumab is a platelet-derived growth factor receptor alpha blocking antibody used with doxorubicin to treat patients with certain types of soft tissue sarcoma (STS).

Olaratumab is indicated, in combination with doxorubicin, for the treatment of adult patients with advanced or mestastatic soft tissue sarcoma (STS) with a histologic subtype for which an anthracycline-containing regimen is appropriate and which is not amenable to curative treatment with radiotherapy or surgery.

Olaratumab is also used to associated treatment for these conditions: Soft Tissue Sarcoma (STS)

How Olaratumab works

Olaratumab blocks ligand-induced tumor cell proliferation, and inhibits receptor autophosphorylation and ligand-induced phosphorylation of the downstream signaling molecules protein kinase B (Akt) and mitogen-activated protein kinase . PDGFR signalling is a type of tyrosine kinase-mediated pathway that normally regulates cell growth, chemotaxis, and mesenchymal stem cell differentiation. It also promotes internalization of PDGFR thus alters the surface levels of PDGFR.

Toxicity

Infusion-related reactions may occur during or after the administration which include bronchospasm, flushing, hypotension, anaphylactic shock, or cardiac arrest. Olaratumab may cause embryo-fetal toxicity based on animal data and its mechanism of action. Other reported adverse effects include neutropenia, leukopenia, anemia, nausea and musculoskeletal pain.

Food Interaction

No interactions found.

Olaratumab Disease Interaction

Moderate: hepatic impairment, renal impairment

Volume of Distribution

7.7 L at steady state.

Half Life

Estimated value of 11 days

Clearance

Mean value of 0.56L/day

Innovators Monograph

You find simplified version here Olaratumab

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