# Novel Long Acting rhTSH Superagonist Analogs for Improved Diagnostic Imaging, Thyroglobulin Stimulation and Therapy of Thyroid Cancer.

> **NIH NIH R44** · TROPHOGEN, INC. · 2020 · $433,685

## Abstract

Thyroid cancer is the most common malignancy of endocrine tissues, disproportionally affecting women, and is
one of the few cancers greatly increasing in incidence & prevalence for unknown reasons. A very aggressive
form of this cancer may result from nuclear accidents like Chernobyl & Fukushima, increasing proximity of
nuclear waste storage sites, or from nuclear explosions including those that could result from well-publicized
terrorist intentions, a vitally important & timely global health problem. Though usually not fatal, most higher risk
patients require lifelong diagnostic surveillance with radioiodine imaging to detect residual tumors requiring
subsequent therapy with 131I to prevent severe, often underestimated morbidity & less common mortality. One
of the PIs (BW), while an intramural lab chief at NIDDK, co-invented, co-developed & licensed to Genzyme
recombinant human (rh)TSH (Thyrogen), with current annual sales over $200 Million. Thyrogen is currently
approved for enhancing imaging with radioiodine, stimulation of the serum marker thyroglobulin (Tg), & normal
thyroid remnant ablation. However, because of its short half-life & lack of equivalent stimulation to thyroid
hormone withdrawal producing hypothyroidism, Thyrogen is not approved for thyroid cancer treatment.
Moreover, there is currently no method to image or treat the increasing number up to 20% of much more
aggressive, more radio-resistant cancers which cause major morbidity and decreased quality of life not totally
reflected in cancer mortality figures. The PIs have previously invented a novel 1st & 2nd generation superagonist
analogs of rhTSH, the earliest non-commercialized drug candidates, of higher potency, initially licensed by the
PIs from NIDDK. The current proposal is related to a totally novel 3rd generation analog, the proposed final drug
candidate, with greatly increased half-life achieved with a totally novel dual neoglycosylation insert that for the
first time synergizes with the superagonist mutations to achieve much higher in vitro & vivo potency, as well as
for the 1st time maximal efficacy in responsive & radio-resistant cancers with fewer, less painful subcutaneous
injections, without any toxicity or immunogenicity. TR14601 or TR14701 greatly superior to Thyrogen, all
previous Trophogen analogs & will allow greatly improved diagnosis and treatment of patients with thyroid
cancer, including many of those currently viewed as radio-resistant for which there is no current therapy.
Trophogen analogs, & thus provides much superior patent protection for major commercialization advantages
over Thyrogen and any possible future biosimilars. We now provide compelling preliminary in vivo imaging &
thyroglobulin (Tg) biomarker stimulation data demonstrating the vast superiority of two newest analogs to
Thyrogen & to 2nd generation analogs in normal thyroid, as well as two novel, highly relevant xenograft tumor
models. We believe these compelling preliminary in vivo imag...

## Key facts

- **NIH application ID:** 10007767
- **Project number:** 5R44CA224376-03
- **Recipient organization:** TROPHOGEN, INC.
- **Principal Investigator:** MARIUSZ WALDEMAR SZKUDLINSKI
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $433,685
- **Award type:** 5
- **Project period:** 2018-08-01 → 2022-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10007767

## Citation

> US National Institutes of Health, RePORTER application 10007767, Novel Long Acting rhTSH Superagonist Analogs for Improved Diagnostic Imaging, Thyroglobulin Stimulation and Therapy of Thyroid Cancer. (5R44CA224376-03). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10007767. Licensed CC0.

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