RZ-402 is a Small Molecule owned by Rezolute, and is involved in 3 clinical trials, of which 2 were completed, and 1 is ongoing.

RZ-402 is a plasma kallikerin inhibitor (PK). PK circulates in plasma as a zymogen, and upon activation cleaves high molecular weight kininogen to generate the vasoactive peptide bradykinin (BK). BK and its metabolites cause the opening of endothelial tight junctions lining blood vessels, resulting in increased vascular permeability. Fluid and macromolecular components of the plasma leak from the vessels into surrounding tissue potentially resulting in formation of edema. Activation of PK leads to increased retinal vascular permeability (RVP). By inhibiting kallikrein, the drug candidate reduces RVP and ameliorates the disease condition.

The revenue for RZ-402 is expected to reach a total of $453m through 2038. This change impacts the valuation of this asset and is an important factor to understand the current value of the drug in a clinical process. View the complete picture with the RZ-402 NPV Report.

RZ-402 was originated by ActiveSite Pharmaceuticals and is currently owned by Rezolute.

RZ-402 Overview

RZ-402 is under development for the treatment of diabetic macular edema (diabetes-induced retinal vascular permeability). It is administered through oral route. The drug candidate targets plasma kallikrein. It was also under development for treatment of intracerebral hemorrhage (hyperglycemia-induced hematoma expansion) and diabetic retinopathy (DR). 

Rezolute Overview

Rezolute formerly, AntriaBio Inc, is a clinical-stage biopharmaceutical company that carries out the development of innovative drug therapies for the treatment of metabolic diseases related to chronic glucose imbalance. Its pipeline product portfolio includes RZ358 which is an intravenous monoclonal antibody. RZ358 is used for the treatment of conditions characterized by excessive insulin levels and is developing to treat hyperinsulinism and low blood sugar characteristic of diseases such as congenital hyperinsulinism. The company also offers RZ402 which is a potent plasma kallikrein inhibitor used for the treatment of diabetic macular edema (DME). Rezolute is headquartered in Redwood City, California, the US.

The operating loss of the company was US$22.4 million in FY2021, compared to an operating loss of US$20.5 million in FY2020. The net loss of the company was US$20.9 million in FY2021, compared to a net loss of US$20.3 million in FY2020.

Quick View – RZ-402

Report Segments
  • Innovator
Drug Name
  • RZ-402
Administration Pathway
  • Oral
Therapeutic Areas
  • Central Nervous System
  • Metabolic Disorders
Key Companies
  • Sponsor Company: Rezolute
  • Originator: ActiveSite Pharmaceuticals
Highest Development Stage
  • Phase II


GlobalData, the leading provider of industry intelligence, provided the underlying data, research, and analysis used to produce this article.

To create this model, GlobalData takes into account factors including patent law, known and projected regulatory approval processes, cash flows, drug margins and company expenses. Combining these data points with GlobalData’s world class analysis creates high value models that companies can use to help in evaluation processes for each drug or company.

The rNPV method integrates the probability of a drug reaching a clinical stage into the cash flow at that time, which provides a more accurate valuation, as it considers the probability that the drug never makes it through the clinical pathway to commercialization. GlobalData’s rNPV model uses proprietary likelihood of approval (LoA) and phase transition success rate (PTSR) data for the indication in the highest development stage, which can be found on GlobalData’s Pharmaceutical Intelligence Center.