Rinatabart sesutecan

Investigational

Rina-S; PRO1184; PRO-1184; PRO 1184; GEN1184; rinatabart sesutecan

Target

Folate receptor alpha (FRalpha) · FOLR1

Sponsor

ProfoundBio / Genmab

Indication

Advanced/recurrent ovarian cancer

Target family

Folate receptor

RP2D dose

120 mg/m2

Q3WRP2D

Multi-organ toxicity

Fingerprint & organ drill-down

Also reported

0%severity100%

Assessed · clear

true 0%

No data

never assessed

4 adverse-event terms

Ocular

Any-grade

G3+

RP2D

sagittal schematic · -

↳

Tissues shaded by reported adverse-event rate.

Cornea

Express.

0.02%

Limbus

Express.

0.07%

Conjunctiva

Express.

0.19%

Lens

Express.

Retina / RPE

Express.

3.21%

0.4 nTPM

Dominant tissue

Surface subtype

None

Reversibility

Reported ocular events

Vision blurred63%

Dry eye37%

Keratopathy33%

Ocular toxicity (any)0%

n=20

Construct

Molecular anatomy

Antibody

IgG1

Humanized

Linker

Cleavable

DAR

Payload

Exatecan

TopoI inhibitor

Linker structureC59H91N15O17

CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N(C)Cc1cc(NC(=O)C(C)NC(=O)C(NC(=O)CCCCCN2C(=O)C=CC2=O)C(C)C)ccc1CO

Payload structureC24H22FN3O4

CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C5[C@H](CCC6=C5C(=CC(=C6C)F)N=C4C3=C2)N)O

Antibody

Antibody & Fc engineering

Antibody

Rinatabart

Isotype

IgG1

Origin

Humanized

Fc modifications

Glycoengineering

Effector silencing

Unknown

FcγR binding

Unknown

C1q binding

Unknown

Linker & conjugation

Linker chemistry

Linker profile

Linker

Cys-11 ADC linker (hydrophilic peptide-maleimide)

Class

Cleavable

Cleavage

Cleavable

Attachment

Cysteine (interchain)

Conjugation

Conventional cys

Symmetry

Symmetric

DAR (mean)

DAR homogeneity

Homogeneous

Plasma t½

Cleavage trigger

Cathepsin B (peptide-cleavable)

Release control

Conditional

Hydrophilicity mask

Hydrophilic-linker

Formula

C59H91N15O17

Linker MW

1282.465 Da

Linker TPSA

368.32 Å²

Linker xLogP

-4.1894

ADCdb linker

LIN0WCLMP

In-vitro stability

Payload

Payload & physicochemistry

Payload profile

Payload

Exatecan

Class

Topoisomerase I inhibitor

Mechanism

TopoI inhibitor

Released catabolite

Exatecan

Mechanistic subtype

TopoI

Stereochem / salt

Bystander

Yes

PAMPA rank

435.4 Da

XLogP3

0.4

logD₇.₄

TPSA

106 Å²

pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

IC50 (HCEC)

Formula

C24H22FN3O4

PubChem CID

151115

ADCdb payload

PAY0LEIGJ

Bioactivity note

Payload exatecan (DX-8951f) is a potent DNA topoisomerase I (TOP1) inhibitor; reported cell-free/enzymatic IC50 ~2.2 uM (0.975 ug/mL) with strong membrane permeability and bystander effect. ADC: FRalpha-directed, homogeneous DAR 8; sesutecan is a hydrophilic, stable, cleavable ex

Dosing & regimen

Dosing

RP2D dose

120 mg/m2

Schedule

Q3W

Route

Fractionated

n at RP2D

Dose basis

BSA

Trial phase

Phase 1/2

Dose-OAE available

Tox summary basis

RP2D

Ocular & expression

Ocular profile & eye-tissue target expression

Target profile

OAE any-grade

0 %

OAE grade 3+

OAE data status

documented-absent

Severity (weighted)

Keratopathy

Conjunctival

Dry eye

Blurred vision

Dominant tissue

Surface subtype

None

Grading scale

CTCAE (unversioned)

Reversibility

Target expression in eye tissues (HCA detection · HPA bulk)

Cornea (central)

0.02 %

Cornea (limbal)

0.07 %

Conjunctiva

0.19 %

RPE

3.21 %

Retina (HPA)

0.4 nTPM

Cross-trial comparability

Ascertainment: Symptom-driven reportingScale: CTCAE (unversioned)Denominator: RP2D⚠ OAE rate not directly comparable across trials

Identity & registry

Identifiers, registry & notes

ADC id

rinatabart-sesutecan

Approval status

Investigational

Approval year

UniProt

P15328

ADCdb ADC

DRG0TUKTY

ADCdb antibody

ANI0RYL006

ADCdb target

TAR0QHAVI

Primary source

Genmab/GlobeNewswire SGO 2026 (RAINFOL-01 D2); ESMO 2024 abstract 719MO (RAINFOL-01 Part A)

Aliases & development codes

Rina-S; PRO1184; PRO-1184; PRO 1184; GEN1184; rinatabart sesutecan

Notes

PRO-1184 = rinatabart sesutecan (Rina-S; PRO1184/GEN1184), an investigational FRalpha (FOLR1)-targeted ADC with an exatecan (topoisomerase I inhibitor / camptothecin analog) payload at DAR 8, conjugated via an interchain-cysteine maleimide on the hydrophilic, cleavable 'Cys-11' peptidomimetic linker (ADCdb LIN0WCLMP). Sponsor: ProfoundBio, acquired by Genmab. Trial: RAINFOL-01 (NCT05579366), Phase 1/2; RP2D 120 mg/m2 IV Q3W. OCULAR ANCHOR (per triage, basis=explicit-zero): Ocular toxicity was explicitly assessed and ABSENT. Verbatim (SGO 2026 combo cohort D2, Genmab/GlobeNewswire 2026-04-13): 'No safety signals of ocular toxicities, peripheral neuropathy or interstitial lung disease were reported.' ESMO 2024 monotherapy data (Part A, 100/120 mg/m2): investigators observed no signs of ocular toxicity, neuropathy, or ILD. oae_any_pct set to 0 with documented note; ocular_surface_subtype=None. This is a clean low/negative control vs antitubulin ADCs (e.g. mirvetuximab-soravtansine DM4 keratopathy). TOXICITY SCOPING: Two cohorts exist. (1) Monotherapy Part A at 120 mg/m2, N=20 (CancerNetwork/OncLive): the cleanest single-agent RP2D dataset -> grade 3/4 anemia 45%, grade 3/4 neutropenia 45% (55% G-CSF use), nausea 70% (G1/2), fatigue 45%, vomiting 40%; G3+ TEAEs 65%. (2) Combination D2 (Rina-S 120 mg/m2 + bevacizumab Q3W), N=40 (SGO 2026): nausea 80%, fatigue 67.5%, anemia 55%, neutropenia 45% - NOT used for per-organ RP2D rows because bevacizumab confounds. RP2D toxicity_rows are anchored on the N=20 monotherapy cohort; per-AE any-grade breakdown supplemented from ESMO 2024 pooled Part A (100/120 mg/m2): nausea 57%, neutropenia 51% (G3 34%), leukopenia 46% (G3 23%), anemia 43% (G3 26%), thrombocytopenia 31% (G3 14%), vomiting 26%. PAYLOAD PHYSCHEM (exatecan, PubChem CID 151115, computed): MW 435.4, XLogP3 0.4, TPSA 106, formula C24H22FN3O4. Charge neutral at pH7.4; bystander-capable (membrane-permeable camptothecin like DXd/SN-38). pKa and logD7.4 left blank (not retrieved from a primary source). LINKER PHYSCHEM (ADCdb LIN0WCLMP): formula C59H91N15O17, MW 1282.465 Da, TPSA 368.32, xLogP -4.1894 (strongly hydrophilic -> hydrophobicity_masking_strategy=Hydrophilic-linker), SMILES recorded. INFERENCE FLAGS / CONSERVATISM: antibody_isotype=IgG1 and antibody_origin=Humanized are inferred (typical for this class; not explicitly stated in retrieved sources - tier C). linker_cleavage=Cathepsin B is the most likely peptide-cleavage mechanism for this hydrophilic protease-cleavable linker but ADCdb labels it 'thiol-sensitive/cleavable' without naming the protease (recorded conservatively). dar_mean=8 and conjugation 'Conventional cys' per ADCdb. fc_modifications/glycoengineering/effector silencing not disclosed (left blank/Unknown). All clinical numbers are conference-abstract / press-release sourced (tier D); no FDA label or peer-reviewed full paper exists yet. released_catabolite_identity=Exatecan (free payload after linker cleavage). Per instructions, derived columns (dna_damage subtype, stability conditional/unconditional, FcgammaR/C1q binding, severity, HCA/HPA, oae_data_status) were NOT filled - inputs only.