Our pipeline efforts aim to offer patients and physicians confidence and hope.

PMI05

Drug Candidate
PMI05

Summary
Potential first-in-class imaging agent for CAIX associated cancers

Mechanism of Action
PET/SPECT ligand targeting CAIX

Indication
Oncology

Development Stage
Phase I

 
 

Clear cell renal cell carcinoma (ccRCC) is the most malignant type of RCC, which, in turn, is the most lethal of genitourinary cancers.  Carbonic anhydrase 9 (CAIX) is a well-known target overexpressed in ccRCC, and is already a target for imaging this disease.  But that imaging is done primarily with antibody-based agents.  

We developed the first small-molecule CAIX-targeted imaging agents. This asset is a first-in-class agent for single photon emission computed tomography (SPECT) imaging of CAIX. It is also a prototype for our corresponding 64Cu- and 18F-labeled agents for positron emission tomography (PET) and theranostics based on this scaffold. PMI05 has recently begun a phase 1 clinical trial.

PMI06

Drug Candidate
PMI06

Summary
Potential best-in-class PD-L1 imaging agent for immuno-oncology

Mechanism of Action
PET ligand targeting PD-L1

Indication
Immuno-oncology

Development Stage
Phase I

 
 

Arguably the greatest advance in cancer therapy in recent memory has been the introduction of immune checkpoint inhibitors to the clinic. The 2018 Nobel Prize in Physiology or Medicine went to individuals who discovered the phenomenon of immune checkpoint inhibition. Similar to other PD-L1 compounds we have published, we have developed a radiofluorinated, peptide-based imaging agent for detecting the PD-L1 checkpoint in vivo with positron emission tomography (PET). PD-L1 is present in tumors and certain immune cells. Unlike antibody-based agents for imaging PD-L1, this agent can be used within standard clinical workflow. In addition to detecting PD-L1, this agent can be used to calculate the amount of anti-PD-L1 therapeutic antibody that arrives at its target, and can also provide an indirect readout of PD-1 engagement by therapeutic antibodies. This compound will be synthesized in a cyclotron facility and distributed ready to inject. PMI06 has recently begun a phase 1 trial in non-small cell lung cancer.

PMI06-G

Drug Candidate
PMI06-G

Summary
Potential best-in-class PD-L1 imaging agent for immuno-oncology

Mechanism of Action
PET ligand targeting PD-L1

Indication
Immuno-oncology

Development Stage
Preclinical

 
 

PMI06-G is 68Ga labeled version of PMI06 for PET. It is to be used in venues where a cyclotron is remote, and on-site generator production of 68Ga is necessary.

PMI07

Drug Candidate
PMI07

Summary
Potential first-in-class FAP imaging agent for cancer and fibrosis

Mechanism of Action
PET ligand targeting FAP

Indication
Oncology, Fibrosis

Development Stage
Preclinical

 
 

The fibroblast activation protein (FAP) is present in the microenvironment and/or epithelium of a wide variety of cancers. We have developed a series of FAP-targeting radiopharmaceuticals and optical agents.

While PMI07 is the published 111In-labeled SPECT agent, agents radiolabeled with 18F and other imaging radionuclides have been developed, and are progressing toward IND-enabling studies.

PMI21

Drug Candidate
PMI21

Summary
PSMA-targeted alpha medical isotope-based therapeutics

Mechanism of Action
Radiopharmaceuticals

Indication
Prostate cancer

Development Stage
Preclinical-IND enabling

 
 

Small molecules targeting the prostate-specific membrane antigen (PSMA) were originally described by us. PSMA-targeted imaging and therapeutic agents can arguably be said to have revitalize nuclear medicine in recent years, and have contributed significantly to commercial interest in the field. PMI21 is a theranostic radiolabeled with 211At, which we believe to be a less toxic alternative to other alpha-particle-emitting radionuclides. Furthermore, this compound is based on the scaffold designed to avoid binding to off-target tissues such as the salivary and lacrimal glands. A lead agent has been uncovered, and is currently undergoing IND-enabling studies.

  1. Pomper, M. G.; Musachio, J. L.; Zhang, J.; Scheffel, U.; Zhou, Y.; Hilton, J.; Maini, A.; Dannals, R. F.; Wong, D. F.; and Kozikowski, A. P. “11C-MCG: synthesis, uptake selectivity, and primate PET of a probe for glutamate carboxypeptidase II (NAALADase)”. Mol. Imaging. 2021, 1, 96-101.

  2. Foss, C. A.; Mease, R. C.; Fan, H.; Wang, Y.; Ravert, H. T.; Dannals, R. F.; Olszewski, R. T.; Heston, W. D.; Kozikowski, A. P.; Pomper, M. G. “Radiolabeled small-molecule ligands for prostate-specific membrane antigen: in vivo imaging in experimental models of prostate cancer”. Clin. Cancer Res. 2005, 11, 4022-4028.

  3. Banerjee, S. R.; Foss, C. A.; Castanares, M.; Mease, R. C.; Byun, Y.; Fox, J. J.; Hilton, J.; Lupold, S. E.; Kozikowski, A. P.; and Pomper, M. G.; “Synthesis and evaluation of technetium-99m- and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA)”. J. Med. Chem. 2008, 51, 4504-4517.

  4. Banerjee, S. R.; Kumar, V.; Lisok, A.; Chen, J.; Minn, I.; Brummet, M.; Boinapally, S.; Cole, M.; Ngen, E.; Wharram, B.; Brayton, C.; Hobbs, R. F.; Pomper, M. G.; “ 177177Lu-labeled low-molecular-weight agents for PSMA-targeted radiopharmaceutical therapy”. Eur J Nucl Med Mol Imaging 2019, 46, 2545-2557.

  5. Mease, R. C.; Kang, C.; Kumar, V.; Ray, S.; Minn, I. L.; Brummet, M.; Gabrielson, K.; Feng, Y.; Park, A.; Kiess, A.; Sgouros, G.; Vaidyanathan, G.; Zalutsky, M.; Pomper, M. G. “An improved 211At-labeled agent for PSMA-targeted alpha therapy. J Nucl Med 2021 June

  6. Mease RC, Kang C, Kumar V, Ray S, Minn IL, Brummet M, Gabrielson K, Feng Y, Park A, Kiess A, Sgouros G, Vaidyanathan G, Zalutsky M, Pomper MG. “An improved 211At-labeled agent for PSMA-targeted alpha therapy.” Journal of Nuclear Medicine. 2022, 63 (2) 259-267

PMI31

Drug Candidate
PMI31

Summary
Potential first-in-class FAP therapeutics for cancer and fibrosis

Mechanism of Action
Undisclosed

Indication
Undisclosed

Development Stage
Discovery

 
 
 

PMI31 is a radiotherapeutic version of PMI07, which targets FAP. Several different radioisotopes are under investigation and are currently undergoing comparison in relevant preclinical models.