Notes
SHR-A1811 = trastuzumab rezetecan (Aiweida/Avida), China's first domestically developed ADC; NMPA-approved 2025-05-29 for HER2-mutant advanced/metastatic NSCLC (>=2L), basis HORIZON-Lung. Sponsor Jiangsu Hengrui (ex-China: Luzsana). Composition: trastuzumab (humanized IgG1-kappa, anti-HER2) + Mc-GGFG cleavable tetrapeptide linker = LIN0ECMCR, structurally IDENTICAL to the deruxtecan linker shared with T-DXd and Dato-DXd in the DB (linker physchem carried from that shared ADCdb/PubChem entry: C25H31N5O8, MW 529.55, TPSA 191.08, xLogP -1.3675) + rezetecan (SHR9265/SHR169265), a DISTINCT exatecan-derived TopoI inhibitor (chiral cyclopropyl at the carbonyl alpha-position; MW 533.55; LogD7.4 1.89; ALogP 3.67; membrane Peff ~5x DXd; bystander-positive) -- so payload values were taken from the SHR-A1811 characterization paper, NOT copied from DXd. DAR ~5.7 (ADCdb measured range 5.3-6.4; design-nominal ~6). In-vitro stability <2% payload release at 21 d in human plasma (>98% retained). OCULAR (the qualifying signal, kept conservative): China NMPA pooled 3-trial label lists blurred vision as 'common' (CIOMS band ~1-10%; no published point estimate) with conjunctival hyperaemia and lacrimation increased 'infrequent' (~0.1-1%); global Ph1 HORIZON-X reported 1 grade-3 ulcerative keratitis among 30 non-Asian pts at 4.8 mg/kg (3.3%). The NSCLC Ph1/2 (N=63) and pivotal HORIZON-Lung (N=94) AE tables listed NO ocular AEs, so blurred vision is recorded only qualitatively in the ocular group (band, not a fabricated numeric row); the single numeric ocular toxicity row is the G3 keratitis. Frontiers 2026 review notes no reversibility data and no post-marketing ocular reports for this drug. TOXICITY pattern is hematologic-dominant: pivotal HORIZON-Lung (N=94, 4.8 mg/kg, CTCAE v5.0) G3+ -> neutropenia 40%, WBC decreased 27%, anaemia 23%, thrombocytopenia 11%, lymphopenia 7% (overall G3+ TRAE 62%); the any-grade panel is from the same NSCLC program reported earlier as Ph1/2 (N=63, CTCAE v5.0) -> neutropenia 79.4%, anaemia 76.2%, WBC 73.0%, platelets 42.9%, nausea 79.4%, vomiting 60.3%, decreased appetite 55.6%, fatigue/asthenia 60.3%, alopecia 41.3%, ALT 42.9%, AST 39.7%, bilirubin 14.3% (hepatic transaminitis all low-grade, 0 G3+). ILD is the key class risk: ~11.6% (5/43) low-grade at RP2D, 11.1% (7/63) whole NSCLC cohort including 1 G5 fatal in the higher 6.4 mg/kg cohort (no fatal ILD at RP2D), vs 2.5% across all tumors in global Ph1 (N=307). Peripheral neuropathy and infusion-related reactions were not reported (consistent with the DXd/TopoI class) -> left blank. Caveats recorded in cells: payload charge +1 is inferred (tier C) from the conserved exatecan primary amine; payload TPSA/pKa left blank (not measured for SHR169265); the payload_xlogp3 cell holds the paper's ALogP (3.67), not a PubChem XLogP3. Fatigue/asthenia and alopecia are documented but omitted from toxicity_rows because they fall outside the fixed organ_system enum. CTCAE v5.0 throughout. Note ADCdb labels approval as 'FDA Approval May 2025' but the actual regulatory action was China NMPA (2025-05-29); recorded as NMPA-approved.