Drug intelligence / Profile preview

[225Ac]Ac-Macropa-pertuzumab-PEG6-DM1

Development stage
Preclinical
Lead developer
University of Saskatchewan
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**[225Ac]Ac-Macropa-pertuzumab-PEG6-DM1** is a preclinical HER2-targeted antibody-drug radioconjugate for HER2-positive breast cancer. It consists of the anti-HER2 monoclonal antibody pertuzumab conjugated through a PEG6 linker to the maytansinoid microtubule inhibitor DM1 and labeled with the alpha-particle-emitting radionuclide actinium-225 through the Macropa chelator. Pertuzumab directs the construct to HER2-expressing cells and inhibits HER2 dimerization; intracellular DM1 contributes microtubule disruption, while actinium-225 delivers high-linear-energy-transfer alpha radiation. In mouse xenograft studies, the agent showed activity against trastuzumab-resistant and T-DM1-resistant HER2-positive breast cancer models, with complete remissions in HCC1954 tumors and substantial growth inhibition in JIMT-1 tumors. ([pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/41946831/))

Other names
[225Ac]Ac-Macropa-P-PEG6-DM1[225Ac]Ac-Macropa-pertuzumab-PEG6-DM1
02

Targets

TUBB (Tubulin (alpha and beta subunits))DNAERBB2 (Erb-b2 receptor tyrosine kinase 2)

Beyond the preview

Go deeper on [225Ac]Ac-Macropa-pertuzumab-PEG6-DM1.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Full profile access

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Full profile access

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Full profile access

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Full profile access

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Full profile access

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Full profile access

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on [225Ac]Ac-Macropa-pertuzumab-PEG6-DM1.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call