Table 2.

Aptamer.

No	Study registration number (ref)	Study Population	Age Group	Intervention Arm	n	Comparator arm	n	Time to follow Up	Primary Endpoint	Outcome: Mean Difference (Treatment vs Placebo)	Adverse Events
1	10.1093/eurheartj/ehs232 NCT00932100 (Povsic, TJ et al., 2013)	Non-ST-elevation ACS patients with planned early cardiac catheterization via femoral access <24h. Past medical history of CHF, MI, Previous PCI, Previous CABG, HTN, T2DM, Renal Insuficiency, Stroke, Current tobacco use.	25–75 years old	Pegnivacogin 1 mg/kg and Anivamersen reversal 0.075, 0.20, 0.40, 1.00 mg/kg	REG1 25–100% (n = 40,113,119,194)	Heparin	161	30 days	Primary endpoint: total ACUITY bleeding. Secondary endpoints: major bleeding and ischaemic event.	Total bleeding (%) 33.7, 2.7, 3.7, −1.3; Major bleeding (%) 10, 1, −2, −3; Ischaemic event (%) −2.7 (0.2,1.4)	REG1 n = 60. Heparin n = 55. 3 incidence of allergic-like adverse events within 24 h of drug administration, 2 of 3 are SAE. REG 1 (hives 0.2%, hypotension 2.4%, rash 0%, dyspnoea 0.9%). Heparin (hives 0%, hypotension 1.9%, rash 0.7%, dyspnoea 0%)
2	10.1177/1076029610384114 (Arzamendi D et al., 2011)	CAD patient on double antiplatelet therapy and normal volunteers (CAD patient n = 27 (Male (n = 22), Hypertension (n = 9), Hypercholestrolemia (n = 16), T2DM (n = 4), Smoker (n = 10), ACS (STEMI n = 17; NSTEMI n = 1; UA = 9)), Healthy volunteers n = 5)	18–75 years old	exvivo treated pretherapy (incubated 5 min before the onset of perfusion) or 10 min posttherapy on damaege arteries with: ARC1779 (25, 83, and 250 nmol/L), or Abciximab (100 nmol/L), or placebo	n = 27	placebo	n	15 min	Platelet function	Platelet adhesion: Pretherapy with ARC1779 or Abciximab in patients taking ASA and CPG (n CAD = 17) effect on platelet adhesion (unit: platelets × 10^6/cm2). ARC1779 83 nmol/L: 4.8 (p < 0.05) ARC1779 250 nmol/L: 3.8 (p < 0.05) Abciximab 100 nmol/L: 2.9 (p < 0.05) Placebo: 7.3 (p < 0.05) Pretherapy with placebo in healthy patient (n = 5) effect on platelet adhesion: 81.9 ± 23.6 × 10^6 platelets/cm2 Posttherapy with ARC1779 in CAD (n = 10) p > 0.05 in platelet adhesion compared to placebo. Platelet aggregation Abciximab abolished platelet aggregation in response to TRAP-1, ADP, and AA both in healthy volunteers and in patients. Collagen-induced aggregation: in healthy volunteers; averaged 18 Ω reduce to 2 Ω with abciximab, but unaffected by ARC1779 (18 Ω) in CAD patient; reduced to 3 Ω by abciximab, and unaffected by ARC1779 (4 Ω) Platelet activation This was done on blood samples from healthy volunteers after the perfusion experiments. Neither abciximab nor ARC1779 has a significant effect on P-selectin or vWF expression. Platelet−leukocyte binding increased after blood perfusion (control) compared with nonperfused blood (baseline), not significantly affected by ARC1779 or abciximab.
3	10.1177/2048872617703065 (Staudacher DL et al., 2019)	Healthy volunteers and patient with ACS	≥18 years old (whole blood sample)	Pegnivacogin or Pegnivacogin 1 mg/kg + Anivamersen (RNA Aptamer reversal agent)	n	Placebo	n	20 min	CD62P-expression, PAC-1 binding	Pegnivacogin when compared with placebo CD62P expression 20 mikroM ADP (n = 9): -13.38 p = 0.027 1 mikroM ADP (n = 24): -6.59 p = 0.031 PACbinding 20 mikroM ADP (n = 11): -16.98 p = 0.0098 1 mikroM ADP (n = 25): -9.59 p = 0.0008 Pegnivacogin effect on ADP-activated platelets could be completely negated by Anivamersen, compared with Placebo CD62P expression 20 mikroM ADP (n = 10): -2.42 p = 0.922 1 mikroM ADP (n = 3): -2.38 p = 0.449 Blood from healthy subject after ex-vivo incubation with 150 μl pegnivacogin: platelet aggregation −3.66% p = 0.002, n = 10 Patient CAD treated dual antiplatelet after 20min iv 1 mg/kg pegnivacogin: platelet aggregation −56.79% p = 0.020, n = 3
4	10.1161/CIRCULATIONAHA.107.745687 (Chan, MY et al., 2008)	Subjects with stable CAD	50–75 years old	aptamer (RB006) sd 1 min iv ASO (RB007) sd 3h iv	Group 1 = 28; 6,6,8,8 (RB006 15,30,50,75 mg with RB007 30,60,100,150 mg) Group 2 = RB006+Placebo antidote = 14; 3,3,4,4	placebo	8	day 7	safety, tolerability, pharmacodynamic	RB006 increased the activated partial thromboplastin time dose dependently; the median activated partial thromboplastin time at 10 min after a single intravenous bolus of 15, 30, 50, and 75 mg RB006 was 29.2, 34.6, 46.9, and 52.2 s, P < 0.0001. RB007 reversed the activated partial thromboplastin time to baseline levels within a median of 1 minute with no rebound increase through 7 days.	No major bleeding. 10% experienced non–dose-dependent and mainly mucocutaneous bleeding.
5	NCT00715455	undergo non-urgent PCI have a prior indication for PCI pre-treatment with aspirin and CPG	18–80 years old	RB006 1 mg/kg/IV, SDRB007 0.2:1 (50% efficacy)/2:1 (100%), SD	20	UFH IV treated	4	48 hours 14 days	major bleeding 48 h/hospital discharge all-cause death, MI-event, urgent revasc 14 days	1.0 Median (0.9, 1,1) p < 0.001	A total of 4 AEs, 2 patients from treatment group2 patients from control/comparison group