Table 4 AsiDNA pharmacokinetic parameters after the first and the third administration of AsiDNA by IV (1-h infusion) route from DL1 to DL5.

From: A Phase 1 dose-escalation study to evaluate safety, pharmacokinetics and pharmacodynamics of AsiDNA, a first-in-class DNA repair inhibitor, administered intravenously in patients with advanced solid tumours

AsiDNA cycle 1 day 1

AsiDNA cycle 1 day 3

Median [minimum–maximum]

Median [minimum–maximum]

Dose (mg)

Cmax (ng/mL)

tmax (h)

AUClast (ng.h/mL)

CL (L/h)

Cmax (ng/mL)

tmax (h)

AUClast (ng.h/mL)

CL (L/h)

200

42,123 [38,449–55,836]

1.25 [0.917–1.35]

96,596 [82,078–128,652]

1.98 [1.55–2.40]

36,035 [32,693–45,408]

0.917 [0.917–1.20]

94,118 [55,170–118,842]

1.68 [1.68–1.68]

400

71,471 [38,480–119,060]

0.917 [0.500–1.22]

110781 [89,445–236,239]

3.69 [1.67–4.44]

75,442 [64,639–99,393]

0.917 [0.917–0.917]

127,462 [102,909–220,713]

3.14 [1.81–3.89]

600

137,342 [82,802–143,747]

0.917 [0.467–0.950]

254,672 [162,437–256,918]

2.35 [2.32–3.65]

141,138 [123,206–147,954]

0.950 [0.933–0.950]

237,224 [232,150–238,259]

2.53 [2.52–2.58]

900

150835 [91,279–393,534]

1.01 [0.500–1.28]

311,105 [161,129–520,430]

2.90 [1.73–5.55]

179,338 [126,930–285,174]

0.983 [0.917–1.25]

246,037 [204,358–385,973]

3.66 [2.33–4.40]

1300

375847 [338,946–618,618]

0.934 [0.567–1.25]

515,015 [382,229–822,747]

2.51 [1.58–3.39]

404,071 [231,811–512,882]

0.942 [0.917–0.967]

498,370 [298,665–684,756]

2.63 [1.90–4.35]

  1. Blood samples for PK analysis were collected from 22 patients. Of note, for 2 subjects who received AsiDNA 200 mg, samples were missing at 23 h after the third infusion, and 1 patient receiving AsiDNA 900 mg had issues during the third infusion, therefore this patient was not included in the analysis.
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