On April 23, 2026 Transcenta Therapeutics (HKEX: 06628), a global clinical stage biopharmaceutical company with fully-integrated capabilities in discovery, research, development and manufacturing of antibody-based therapeutics, reported the presentation of preclinical data highlighting its proprietary LIV1-targeting antibody-drug conjugates (ADC) at the 2026 AACR (Free AACR Whitepaper) Annual Meeting. The data demonstrate strong anti-tumor activity, differentiated payload-dependent efficacy, and favorable tolerability profiles, supporting further development in LIV1-positive solid tumors.
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LIV1 is a member of the zinc transporter family, with limited normal tissue expression, and is found to be overexpressed with high prevalence in breast (93%), prostate (72%) and lung (10%) cancers, making it an attractive cell surface target for developing ADC therapeutics.
Transcenta Therapeutics has developed 48D6, a novel proprietary humanized anti-LIV1 monoclonal antibody with high affinity, specificity, and internalization capability. Using Retrogenix cell microarray technology, 48D6 demonstrated no non-specific interactions with other human proteins, confirming its high target specificity. Leveraging 48D6, Transcenta Therapeutics then generated two ADC candidates using a glycotransferase-mediated site-specific conjugation platform: ADC-2, conjugated with a Topoisomerase I inhibitor payload, and ADC-3, conjugated with MMAE.
Pharmacokinetic studies in Balb/c mice showed that ADC-2 exhibited a half-life of approximately 10.4–11.6 days, significantly longer than that of a benchmark SGN-LIV1A analog (3.7–3.9 days), and comparable to the naked antibody 48D6 (13.8–15.6 days), indicating favorable in vivo stability.
In vivo efficacy studies demonstrated that ADC-2 elicited potent anti-tumor activity in LIV1-expressing ER+/HER2- breast cancer and non-small cell lung cancer (NSCLC) patient-derived xenograft (PDX) models at a dose of 6 mg/kg administered once weekly for four weeks.
For LIV1 expressing prostate PDX models, ADC-2 demonstrated limited tumor growth inhibition after two doses. After MMAE-based ADC-3 replaced ADC-2 from the 3rd dose, ADC-3 inhibited the growth of the prostate tumor significantly. In a LIV1 high expressing prostate PDX, the tumor growth was suppressed by ADC-3 for more than 70 days after the dosing was stopped.
In exploratory toxicity studies to assess safety and tolerability, ADC-2 was well tolerated following repeated administrations in mice at all doses tested. Slight lesions were observed in 60 mg/kg group during the treatment period and fully recovered at the end of the recovery period. Based on these results, the maximum tolerated dose (MTD) of ADC-2 in mice was determined at 60 mg/kg. The safety and tolerability of ADC-3 has not yet been explored.
Collectively, these data demonstrate that Transcenta’s LIV1-targeting ADC-2 and ADC-3 programs exhibited strong anti-tumor activities as monotherapy in PDX models of ER+/HER2- breast cancer (representing ~60% of all breast cancers) and also prostate cancer. ADC-2 also displayed excellent tolerability profile in mice. Notably, Transcenta’s LIV1-targeting ADCs also demonstrated potent anti-tumor activity in triple-negative breast cancer (TNBC) tumor models, with data previously presented at the 2024 SABCS. These results support further investigation of Transcenta’s LIV1 ADCs in LIV1-positive solid tumors.
(Press release, Transcenta, APR 23, 2026, View Source [SID1234664742])